dooq Bioscience the Benchmark in Inhibitors From Experience to Insight Inhibitors Catalog

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1 dooq Bioscience the Benchmark in Inhibitors From Experience to Insight Inhibitors Catalog Adooq Bioscience LLC Barranca Parkway, Suite 250 Irvine, CA 92604, USA Phone: Fax:

2 About Us I Who We Are About Us Adooq Bioscience, located in Irvine of California, is one of the world leading suppliers of high purity inhibitors, chemical probes and reference compounds for research fields. Adooq supplies over 6000 products with in-house validated biological and pharmacological activities, and a unique collection of over 3000 inhibitors on HDAC, PI3K, Apoptosis and more signaling pathways. Our Global Presence Adooq aims to be a leading company in all of the markets and to have the world s most prominent brand. Adooq has more than 25 distributors in 30 different countries all over the world. Our worldwide marketing network supports the first-class service on five continents. Find out about our distributors in each region. Our Technology and Quality Adooq focuses on technologies that improve our ability to find, develop and produce life-science reagents. The quality and effectiveness of all Adooq products have been demonstrated through preclinical research. Our Innovations Innovation plays a key role in our company success. Adooq brings more than 600 new products each year to the market, to help our customers achieve the project. CiteAb recognizes Adooq as the chemical probes company to watch in 2018, which is making the largest gains in the market. We believe all those successes are from new innovations. Our Quick Delivery For U.S. based customers, Adooq provides priority overnight shipping for next day delivery before 10:30 a.m (U.S. local time). Adooq has an established marketing network outside of U. S.. No matter where you are located across the globe, if your purchased items are in stock, Adooq will initiate the shipping process within 24 hours. Our Mission At Adooq, we have always believed in the importance of building a great, enduring company that strikes a balance between profitability and a social conscience. That s why Adooq s employees work to responsibly develop the affordable, reliable life-science reagents the world needs and are committed to continuing to do so. You are welcomed to join or work with us creating innovations that matter to people! sales@adooq.com Phone: Fax:

3 II About Us Distributors III Worldwide Distributors Australia Sapphire Bioscience Pty. Ltd. Tel: Fax: Austria Hölzel Diagnostika Handels GmbH Tel: +49(0) Fax: +49(0) Brazil Biogen Tel: (11) Canada Cedarlane Tel: +1(289) Fax: +1(289) China France Adooq China Tel: CliniSciences Tel: Fax: Czech Republic Germany TATAA Biocenter info@tataa.com Tel: Hölzel Diagnostika Handels GmbH info@hoelzel.de Tel: +49(0) Fax: +49(0) Hongkong ADVANCED TECH. & IND. CO., LTD. mandy@advtechind.com Tel: Fax: Hungary Bio-Science Ltd. bio-sci@bio-science.hu Tel: (06-1) Fax: (06-1) India Biogenuix Medsystems Pvt Ltd contact@biogenuix.com Tel: Fax: Indonesia PT Sciencewerke. enquiry@sciencewerke.com Tel: Fax: Ireland Bioquote Limited sales@bioquote.com Tel: Fax: Israel Israel - BioTag Ltd. info@biotag.co.il Tel: Fax: Israel ENCO Scientific Services info@enco.co.il Tel: Fax: Italy CliniSciences italia@clinisciences.com Tel: Fax: Japan FUNAKOSHI CO., LTD. info@funakoshi.co.jp Tel: Fax: Lebanon DPC/LEBANON SARL info@dpcleb.com Tel: Fax: Malaysia Sciencewerke Sdn Bhd enquiry@sciencewerke.com Tel: Fax: Morocco HexaBiogen maroc@hexabiogen.com Tel: Fax: Trusted by great customers New Zealand Sapphire Bioscience (NZ) Ltd. sales@sapphirebioscience.com Tel: Fax: Singapore Sciencewerke Pte Ltd. enquiry@sciencewerke.com Tel: Fax: Slovak TATAA Biocenter info@tataa.com Tel: South Korea LeehyoBioscience Co., Ltd support@leehyobio.com Tel: Fax: ~3 South Korea Bioclone Corp. bioclone@bioclone.co.kr Tel: Fax: Spain CliniSciences espana@clinisciences.com Tel: Fax: Sweden TATAA Biocenter info@tataa.com Tel: Switzerland Hölzel Diagnostika Handels GmbH info@hoelzel.de Tel: +49(0) Fax: +49(0) Taiwan ASIA BIOSCIENCE CO.,LTD. jimmy@abscience.com.tw Tel: Fax: United Kingdom Bioquote Limited sales@bioquote.com Tel: Fax:

4 IV Contents Contents V Contents Contents Epigenetics...1 HDAC 1 PARP 3 JAK 4 Pim 5 Aurora 5 Sirtuins 6 Epigenetic Reader Domain 7 Histone Demethylases 7 DNA Methyltransferases 8 Histone Acetyltransferases 8 Histone Methyltransferase 8 Apoptosis...9 Bcl-2 Family 9 Caspase 10 p53 11 TNF-alpha 11 IAP 12 MDM2 12 PERK 12 Survivin 13 RIP Kinase 13 ASK 13 c-ret 13 Protein kinase D (PKD) 13 PI3K / Akt / mtor...13 Akt 13 PI3K 14 mtor 17 PDK1 18 DNA-PK 19 RSK 19 GSK-3 19 AMPK 20 MELK 20 ATM / ATR 20 Protein Tyrosine Kinases EGFR / HER2 21 FGFR 23 PDGFR 24 VEGFR 25 IGF-1R 27 FLT3 28 c-met 29 ALK 29 SRC 30 c-kit 31 Tie-2 31 Tyrosine kinase 32 Trk Receptors 32 CSF-1R 32 TAM Receptor 32 Angiogenesis...33 EGFR / HER2 33 FGFR 33 PDGFR 33 VEGFR 33 VDA 33 Ephrin Receptor 33 HIF 33 FLT3 34 ALK 34 BTK 34 FAK 34 Syk 35 BCR-ABL 35 MAPK...36 MEK 36 ERK 37 p38-mapk 38 JNK/c-Jun 39 AP-1 39 Raf 39 TOPK 40 MNK 40 MLK 40 KLF 40 JAK / Stat...40 JAK 40 Stat 40 Pim 41 Cell Cycle...41 Chk 41 CDK 41 Aurora Kinase 43 PLK 43 ROCK 44 c-myc 44 Wee1 44 Ras 44 DYRK 45 G-quadruplex 45 DNA Damage...45 HDAC 45 PARP 45 DNA-PK 45 Topoisomerase 45 Telomerase 46 ATM / ATR 46 DNA, RNA Synthesis 46 RNA/DNA Polymerase 47 DNA alkylator 47 Synthases / Synthetases 47 MTH1 47 Sirtuins 47 IRE1 47 DNA Stain 48 Cytoskeleton...48 Microtubules 48 PAK 48 Dynamin 49 Integrin 49 Kinesin 49 Mps1 49 Gap Junction Protein 49 Cell Metabolism...50 Cytochrome P PPAR 50 PDE 51 HSP 52 Hydroxylases 53 Factor Xa 53 MAO 53 DHFR 54 Dehydrogenases 54 Procollagen C-proteinase 55 Carbonic Anhydrase 55 LXR 55 FAAH 55 CETP 55 Ferroptosis 55 HMG-CoA Reductase 56 FXR 56 IDO 56 Retinoid Receptor 56 Lipase 56 Phospholipases 57 Lipoxygenase 57 AhR 57 NAMPT 57 GLUT 57 Antimetabolite 57 Lipid Metabolism 57 Neuronal Metabolism 57 SREBP 57 LDL 58 Foxo1 58 DGAT 58 Farnesyl Transferase 58 CRM1 58 Thioredoxin 58 Vitamin 58 Decarboxylase 58 Autophagy Signaling...59 Autophagy 59 LRRK2 59 CXCR 59 Immunology & Inflammation. 60 IL Receptor 60 COX 60 CCR 61 Toll-like Receptors 61 CXCR 61 ROS 61 NOS 61 Keap1-Nrf2 61 LTR 62 MALT 62 PD-1/PD-L1 62 NADPH oxidase 62 Immunology & Inflammation related 62 GPCR / G Protein HT Receptors 62 Adrenergic Receptors 63 Histamine Receptors 64 Opioid Receptors 65 Metabotropic glutamate receptors (mglur) 65 Melatonin Receptors 65 Peptide Receptors 65 Smoothened Receptors 65 CXCR 65 G Protein 65 Platelet-Activating Factor (PAF) Receptors 66 Endothelin Receptors 66 LPA Receptor 66 Prostanoid Receptors 66 Adenosine Receptors 66 Cannabinoid Receptors 66 Neurotensin Receptors 67 Orexin Receptors 67 Somatostatin Receptors 67 Neurokinin Receptors 67 Protease-Activated Receptors (PAR) 67 S1P Receptor 67 CGRP Receptor 67 Vasopressin Receptor 68 Sigma receptor 68 Guanylate Cyclase 68 camp 68 GHSR 68 Bombesin Receptors 68 Imidazoline Receptor 68 CCK 68 NF-κB/IkB...68 NF-κB 68 IKK/IκB 69 HDAC 69 TGF-β / Smad...69 TGF-β / Smad Inhibitors 69 Protein Kinase C (PKC) 70 Protein Kinase A (PKA) 71 ROCK 72 Neuronal Signaling 72 β-amyloid 72 γ-secretase 72 Beta-secretase (BACE) 73 COX 73 GABA Receptors 73 NMDA Receptors 74 CaMK 74 AChR 74 P2X Receptor 75 Purinergic (P2Y) Receptors 75 GlyT 75 Proteases...76 Caspase 76 γ-secretase 76 Proteasome 76 HCV Protease 76 HIV Protease 77 DPP-4 77 Cysteine protease 78 Serine Protease 78 Aminopeptidase 78 Thrombin 78 MMP 78 Urokinase 79 Tyrosinase 79 Carboxypeptidases 79 Glutaminase 79 Elastases 79 Microbiology...80 Reverse Transcriptase 80 Integrase 80 HCV Protease 80 HIV Protease 80 CCR 80 Antifection 80 Stem Cells / Wnt...81 Hedgehog 81 Wnt 81 β-catenin 82 Casein Kinase 82 Smoothened 82 GSK-3 82 Hippo 83 Membrane Transporters/Ion Channels...83 ATPase 83 CFTR 83 γ-secretase 83 Calcium Channels 83 Sodium Channels 84 Potassium Channels 84 Chloride Channels 85 SGLT 85 Monocarboxylate transporters (MCT) 85 AMPA receptor 85 P-gp 85 CRM1 85 TRP Channel 86 TRPV 86 Glutamate (EAAT) Transporters 86 Serotonin Transporter 86 Proton Pump 86 OCT 86 NCX 86 Endocrinology / Hormones.86 Estrogen Receptors 86 Progesterone Receptors 87 Androgen Receptors 87 GPR 87 5-alpha-reductase 88 Pregnane X Receptors 88 renin-angiotensin-aldosterone system (RAAS) 88 Aromatase 89 Glucocorticoid receptors 89 Vitamin D Receptors 89 GnRH receptor 89 ROR 89 Transferases...89 Acyltransferases 89 Phosphorylases 89 Ubiquitin...89 E1 activating 90 E2 conjugating 90 E3 ligase 90 DUB 90 p97 90 CRISPR...90 Others...91

5 1 Epigenetics Epigenetics 2 Epigenetics A10560 MC1568 A11920 Romidepsin (FK228,Depsipeptide) Cell cycle, 2014, 13(18), HDAC International journal of cancer, 2014, 135(11), Romidepsin purchased from Adooq MC1568 purchased from Adooq The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Name HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2 Belinostat IC50: 27 nm CUDC-101 IC50: 4.4 nm IC50: 4.5 nm IC50: 12.6 nm IC50: 9.1 nm Droxinostat IC50: 16.9 μm IC50: 13.2 nm IC50: 11.4 nm IC50: 5.1 nm IC50: 2.47 μm IC50: 373 nm IC50: 79.8 nm IC50: 67.2 nm IC50: 1.46 μm IC50: 26.1 nm Givinostat IC50: 7.5~16 nm IC50: 10 nm Dacinostat IC50: 32 nm Panobinostat IC50: 5~20 nm MC1568 IC50:0.1 ~3.4 μm Mocetinostat IC50: 0.15 μm IC50: 0.29 μm Entinostat IC50: 0.51 μm Abexinostat Ki: 7 nm Pracinostat IC50: 49 nm Trichostatin A IC50: ~1.8 nm Ki: 19 nm IC50: 96 nm IC50: 1.66 μm IC50: 1.7 μm Ki: 8.2 nm IC50: 43 nm IC50: 56 nm IC50: 47 nm Ki: 17 nm Tubacin IC50: 4 nm Vorinostat IC50: ~10 nm AR-42 IC50: 30 nm Tubastatin A HCl IC50: 16.4 μm IC50: μm IC50: 137 nm IC50: 15 nm Tubastatin A IC50: 15 nm PCI IC50: 4 μm CUDC-907 IC50: 1.7 nm M344 IC50: 100 nm BG45 IC50: 2 μm Romidepsin IC50: 36 nm Ricolinostat IC50: 58 nm Tacedinaline IC50: 0.9 μm Resminostat IC50: 42.5 nm Tasquinimod Scriptaid RG2833 Ki: 32 nm IC50: 5.0 nm IC50: 2.2 μm IC50: 47 nm IC50: 48 nm IC50: 0.9 μm IC50: 1.8 nm IC50: 289 nm IC50: 51 nm IC50: 1.2 μm IC50: 50.1 nm Ki: 5 nm RGFP966 IC50: 80 nm Nexturastat A IC50: 409 nm IC50: 7 μm TMP269 IC50: 157 nm HPOB IC50: 2.9 μm IC50: 4.4 μm IC50: 1.7 μm IC50: 2.9 μm IC50: 674 nm IC50: 27 nm IC50: 5 μm IC50: 97 nm LMK-235 IC50: 11.9 nm IC50: 4.2 nm 4SC-202 IC50: 1.20 μm IC50: 1.12 μm BRD73954 IC50: 9 μm CAY10603 IC50: 271 nm A10122 A10246 A10337 A10488 A10492 A10516 A10518 Belinostat (PXD101) CUDC-101 Droxinostat ITF2357 (Givinostat) JNJ LAQ824 (NVP-LAQ824) LBH589 (Panobinostat) IC50: 0.57 μm IC50: 4.7 nm IC50: 71.8 nm IC50: 5 nm IC50: 56 nm IC50: 36 nm IC50: 2 pm IC50: 426 nm IC50: 1.4 μm IC50: 43 nm IC50: 280 nm IC50: 140 nm IC50: 70 nm IC50: 854 nm IC50: 10 nm IC50: 100 nm IC50: 191 nm IC50: 2.8 μm IC50: 120 nm IC50: 554 nm IC50: 23 nm IC50: 24 nm IC50: 40 nm IC50: 13 μm IC50: 2.8 nm IC50: 3.0 μm IC50: 0.59 μm IC50: 93 nm IC50: 5.4 nm Med Sci Monit. 2017; 23: LBH589 purchased from Adooq LBH589 is a hydroxamic acid and acts as a non-selective HDAC inhibitor with IC5o of HDAC1 to be 0.23 nm. Available package size: 10,50,100,200mg MC1568 is a member of HDAC inhibitors that inhibits the histone deacetylase class II by modifying the genetic expression of various important genes of cell cycle mostly at G1 phase, resulting in the death of breast cancer cells by apoptosis. Available package size: 10,25,50,100mg A10586 MGCD0103 (Mocetinostat) A10611 MS-275 (Entinostat) A10698 Parthenolide ((-)-Parthenolide) A10700 PCI A10764 Pyroxamide (NSC ) A10830 SB939 ( Pracinostat ) A10947 Trichostatin-A (TSA) Exp Neurobiol Oct; 26(5): Trichostatin-A (TSA) purchased from Adooq Trichostatin A (TSA) inhibits the HDACs 1, 3, 4, 6 and 10 with IC50 values around 20 nm. Available package size: 5,10,25,50mg A10954 Tubacin Sci Rep. 2017; 7: Tubacin purchased from Adooq Tubacin (tubulin acetylation inducer) is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nm. Available package size: 5,10,25,50mg A10979 A11037 A11042 A11152 A11153 A11355 A11361 Vorinostat (SAHA) AR-42 (HDAC-42) Tubastatin A HCl PCI CUDC-907 M344 BG45 CUDC-907 is a single small molecule inhibitor that targets both PI3K and HDAC. CUDC-907 is more efficacious than either a single PI3K or HDAC inhibitor reference compound or a combination of the two single agents at maximally tolerated doses. Available package size: 5,10,50,100mg Romidepsin strongly inhibits HDAC1 and HDAC2 with IC5N/A of 1.6 nm and 3.9 nm, respectively, but is relatively weak in inhibiting HDAC4 and HDAC6 with IC5N/A 25 nm and 79N/A nm, respectively. Available package size: 5,10,25,50mg A11940 ACY-1215 (Rocilinostat) A11964 CI994 (Tacedinaline) A12556 Resminostat A12616 Tasquinimod A12722 Scriptaid A12745 Apicidin A12758 ACY-241 A12911 BRD9757 A13139 RG2833 (RGFP109) A13218 RGFP966 A13405 HDAC inhibitor A14032 Nexturastat A A14128 TMP 269 A14197 HPOB A14221 Splitomicin A14236 Santacruzamate A A14326 TMP 195 A14341 LMK-235 A SC-202 A14418 ST7612AA1 A15220 Resminostat hydrochloride A15354 KD 5170 A15355 NCH 51 A15356 NSC 3852 A15357 TC-H 106 A15387 TCS HDAC6 20b A15437 R A15489 BRD73954 A15781 UF010 A15934 ACY-738 A15935 A16127 A16431 BML-210 ITSA-1 CAY10603 ACY-738 is a potent and selective HDAC6 inhibitor with improved brain bioavailability. ACY-738 inhibits HDAC6 with low nanomolar potency and a selectivity of 60- to 1500-fold over class I HDACs. Available package size: 5,10,25mg

6 3 Epigenetics Epigenetics 4 PARP The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name PARP PARP1 PARP2 PARP3 V-PARP Tankyrase-1 4-HQN IC50: 9.5 μm A Ki: 1 nm Ki: 1.5 nm AG (Rucaparib) 1.4 nm AG Ki: <5 nm AZD2461 Benzamide IC50: 3.3 μm BGP-15 BYK pic50: 7.35 pic50: 5.38 BYK pic50: 8.36 pic50: 7.5 DR 2313 IC50: 0.20 μm IC50: 0.24 μm EB 47 IC50: 45 nm Iniparib INO-1001 IC50: <50 nm ME0328 IC50: 6.3 μm IC50: 0.89 μm Niraparib IC50: 3.8 nm IC50: 2.1 nm IC50: 1.3 μm IC50: 330 nm IC50: 570 nm NU1025 IC50: 400 nm Olaparib IC50: 5 nm IC50: 1 nm IC50: 1.5 μm PJ34 EC50: 20 nm PJ34 HCl EC50: 20 nm Rucaparib Ki: 1.4 nm Talazoparib IC50: 0.58 nm UPF 1069 IC50: 8.0 μm IC50: 0.3 μm Veliparib Ki: 5.2 nm Ki: 2.9 nm A10019 A A10026 A10045 ABT-888 (Veliparib) AG (Rucaparib) Oncotarget Nov 28; 8(61): ABT-888 purchased from Adooq ABT-888(Veliparib) is a potential anti-cancer drug acting as a PARP inhibitor. Available package size: 10,50,100,200mg AG (Rucaparib) is a PARP inhibitor that inhibits poly(adpribose) polymerase (PARP) is a key enzyme in DNA repair. Available package size: 5,25,50,100mg A10046 A10111 AG14361 Olaparib (AZD2281) BMC Cancer201717:638 Olaparib (AZD2281) purchased from Adooq Olaparib (AZD2281) is an inhibitor of poly ADP ribose polymerase (PARP), an enzyme involved in DNA repair. Available package size: 10,25,50,100mg A10164 BSI-201 (Iniparib) A10475 INO-1001 A11026 MK-4827 (Niraparib) A11243 BMN673 A11454 TC-E 5001 A12393 AZD-2461 A12665 PJ 34 hydrochloride A12750 UPF 1069 A13731 JW 55 A14182 Rucaparib A14283 WIKI4 A14309 ME0328 A14371 Benzamide A14986 AIM-100 A15024 BMN-673 8R,9S A15215 PJ34 A HQN A15371 BYK A15372 BYK A15373 DR 2313 A15374 EB 47 A15375 NU 1025 A15528 G007-LK A15786 NVP-TNKS656 A15873 AZ6102 A15927 MN-64 A16344 BGP-15 JAK The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name JAK1 JAK2 JAK3 Tyk2 Other AG-490 IC50: ~10 μm EGFR,ErbB2 AT9283 IC50: 1.2 nm IC50: 1.1 nm IC50: 1 nm-10 nm Aurora B,Aurora A,Abl1 AZ 960 IC50: <3 nm AZD1480 IC50: 0.26 nm Baricitinib IC50: 5.9 nm IC50: 5.7 nm IC50: 53 nm BMS IC50: 360 nm IC50: 1.1 nm IC50: 75 nm IC50: 66 nm CEP IC50: 1.8 nm Cercosporamide IC50: 31 nm Mnk2, Mnk1 Cerdulatinib IC50: 12 nm IC50: 6 nm IC50: 8 nm IC50: 0.5 nm ARK5,MST1,Fms Curcumol Decernotinib IC50: 11 nm Ki: 13 nm Ki: 2.5 nm Ki: 13 nm Fedratinib IC50: 3 nm FLT3,RET Filgotinib IC50: 10 nm IC50: 28 nm IC50: 810 nm IC50: 116 nm FLLL32 IC50: <5 μm Gandotinib IC50: 19.8 nm IC50: 2.52 nm IC50: 48.0 nm IC50: 44 nm FLT3,FLT4,FGFR2 GLPG0634 analogue Go6976 FLT3,PKCα,PKCβ1 INCB39110 (Itacitinib) JANEX-1 IC50: 78 µm Momelotinib IC50: 11 nm IC50: 18 nm IC50: 155 nm NSC IC50: 60 nm NSC 42834(JAK2 Inhibitor V, Z3) NVP-BSK805 2HCl IC50: nm IC50: ~0.5 nm IC50: nm IC50: nm Pacritinib IC50: 1.28 μm IC50: 19~23 nm IC50: 520 nm IC50: 50 nm FLT3 (D835Y),FLT3 Peficitinib PF (oclacitinib) IC50: 10 nm IC50: 18 nm IC50: 99 nm IC50: 84 nm Pyridone 6 (JAK Inhibitor I) IC50: 15 nm IC50: 1 nm IC50: 5 nm Ruxolitinib IC50: 3.3 nm IC50: 2.8 nm Solcitinib (GSK ) S-Ruxolitinib IC50: 3.3 nm IC50: 2.8 nm IC50: 428 nm IC50: 19 nm TCS IC50: 1017 nm IC50: 2550 nm IC50: 8 nm IC50: 8055 nm TG IC50: 6 nm IC50: 169 nm RET,FLT3 Tofacitinib Citrate IC50: 112 nm IC50: 20 nm IC50: 1 nm ROCK2,LCK WHI-P154 IC50: 1.8 μm EGFR,Src,VEGFR WHI-P97 WP1066 IC50: 2.3 μm STAT3 XL019 IC50: nm IC50: 2.2 nm IC50: nm IC50: nm PDGFRβ,FLT3,c-Kit ZM pic50: 4.4 nm pic50: 7.1 nm TGM2, EGFR ZM HCl pic50: 4.4 pic50: 7.1 TGM2,EGFR ZM IC50: 4.7 nm IC50: 6.8 nm STAT-5, EGFR, CDK4 A10047 A10095 A10104 A10110 A10241 A10247 A10263 AG-490 AT9283 AZ-960 AZD1480 CP (Tofacitinib citrate) Curcumol Cyt387 (Momelotinib) CYT387 is an inhibitor of Janus kinases JAK1 and JAK2, acting as an ATP competitor with IC50 values of 11 and 18 nm, respectively. Available package size: 10,25,50,200mg A10546 A11041 LY (Gandotinib) INCB (Ruxolitinib) INCB is a potent and selective inhibitor of Janus-associated kinase (JAK) 1 and 2, with IC50 to be 2.7, 4.5 and 332 nm for JAK1, JAK2 and JAK3 respectively. Available package size: 5,10,25,100mg A11082 A11180 A11193 A11241 TG TG NVP-BSK805 BMS

7 5 Epigenetics Epigenetics 6 A11329 Baricitinib (LY ) A16226 NS-018 maleate A10448 Hesperadin A11608 WHI-P97 A16227 ZM39923 The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do A11795 A11962 A12394 WP1066 TG-02 (SB1317) XL019 A12419 Go 6976 A12694 A12808 A13082 Pacritinib (SB1518) CEP33779 PF (oclacitinib) J Pharmacol Exp Ther Sep; 354(3): PF (oclacitinib) purchased from Adooq PF (oclacitinib) is a potent JAK1 inhibitor. Available package size: 5,10,25,50mg A13162 GLPG0634 Arthritis Rheumatol Apr; 67(4) GLPG0634 purchased from Adooq GLPG0634 is an orally-available, selective inhibitor of JAK1 (Janus kinase 1) being developed by Galapagos for the treatment of rheumatoid arthritis and potentially other inflammatory diseases. Available package size: 5,10,25,50mg A13457 Pyridone 6 (JAK Inhibitor I) A13509 ZM HCl A14012 Decernotinib A14049 WHI-P 154 A14132 NSC 42834(JAK2 Inhibitor V, Z3) A14147 PRT (Cerdulatinib) A14210 Cerdulatinib A14232 Filgotinib A14390 INCB39110 (Itacitinib) A14405 Solcitinib (GSK ) A14438 Peficitinib (ASP015K, JNJ ) A14955 S-Ruxolitinib A15014 Baricitinib phosphate A15056 CYT387 sulfate salt A15134 JANEX-1 A ,2,3,4,5,6-Hexabromocyclohexane A15362 Cercosporamide A15363 Cucurbitacin I A15364 SD 1008 A15365 TCS A15366 ZM A15389 NSC A15911 FLLL32 A15937 CHZ868 A16224 NS-018 A16225 NS-018 hydrochloride Pim The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name Pim1 Pim2 Pim3 Other AZD1208 IC50: 0.4 nm IC50: 5 nm IC50: 1.9 nm CX-6258 IC50: 5 nm IC50: 25 nm IC50: 16 nm CX-6258 HCl IC50: 5 nm IC50: 25 nm IC50: 16 nm PIM-1 Inhibitor 2 Ki: 91 nm SGI-1776 free base IC50: 7 nm IC50: 363 nm IC50: 69 nm FLT3 SMI-4a IC50: 17 nm TCS PIM-1 1 IC50: 50 nm TCS PIM-1 4a IC50: 7 nm IC50: 100 nm A10838 A11945 A11967 A12896 A13203 Aurora A10004 SGI-1776 (free base) SMI-4a TCS PIM-1 4a CX-6258 AZD1208 MLN8237 (Alisertib) SIM-4a is a Pim kinase inhibitor that blocks mtorc1 activity via activation of AMPK. Mostly potent to Pim-2, does not significantly inhibit any other serine/ threonine- or tyrosine-kinases. Available package size: 10,25,50,100mg AZD1208 is orally available, small molecule inhibitor of PIM kinases with potential antineoplastic activity. Available package size: 5,10,25,50mg A14275 CX-6258 HCl A14420 LGB-321 HCl A15055 CX-6258 hydrochloride hydrate A15368 PIM-1 Inhibitor 2 A15369 TCS PIM-1 1 PNAS Dec 13; 113(50): MLN8237 (Alisertib) purchased from Adooq MLN8237 (Alisertib) is a selective Aurora A inhibitor with IC50 of 1.2 nm in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Available package size: 5,10,50,200mg Inhibitor Name Alisertib IC50: 1.2 nm Aurora A Aurora B Aurora C Other IC50: nm AMG-900 IC50: 5 nm IC50: 4 nm IC50: 1 nm p38α, TYK2, JNK2 AT9283 IC50: ~3.0 nm IC50: ~3.0 nm JAK3, JAK2, Abl1 (T315I) Aurora A Inhibitor I IC50: 3.4 nm IC50: 3.4 μm IC50: 432 nm Barasertib IC50: 1368 nm IC50: 0.37 nm BI IC50: 25 nm IC50: 3 nm IC50: 15 nm CCT IC50: 42 nm IC50: 198 nm IC50: 227 nm CCT IC50: 15 nm IC50: 25 nm IC50: 19 nm CYC116 Ki: 8 nm Ki: 9 nm VEGFR2, FLT3, CDK2/CyclinE Danusertib IC50: 13 nm IC50: 79 nm IC50: 61 nm Abl,TrkA,RET ENMD-2076 IC50: 14 nm IC50: 350 nm FLT3, RET, VEGFR3/FLT4 ENMD-2076 L-()-Tartaric acid IC50: 14 nm IC50: 350 nm FLT3,RET, VEGFR3/FLT4 GSK IC50: 1.1 μm IC50: 3.5 nm IC50: 6.5 nm FLT1,Tie-2,SIK Hesperadin IC50: 250 nm TbAUK1 JNJ IC50: 11 nm IC50: 15 nm CDK2/ CyclinE, CDK2/ CyclinA,CDK1/ CyclinB KW-2449 IC50: 48 nm FLT3 (D835Y), Abl (T315I),FLT3 MK-5108 IC50: nm MK-8745 IC50: 0.6 nm IC50: 280 nm MLN8054 IC50: 4 nm IC50: 172 nm LCK, PKA, CK2 PF IC50: 0.8 nm IC50: 5 nm FLT1,FAK,TrkA PHA IC50: 27 nm IC50: 135 nm IC50: 120 nm FGFR1, PLK1, FLT3 human A3 Reversine IC50: 12 nm IC50: 13 nm IC50: 20 nm adenosine receptor SNS-314 Mesylate IC50: 9 nm IC50: 31 nm IC50: 3 nm TAK-901 IC50: 21 nm IC50: 15 nm JAK3,c-Src,YES1 Tozasertib Ki app: 0.6 nm Ki app: 18 nm Ki app: 4.6 nm Bcr-Abl,FLT3 ZM IC50: 110 nm IC50: 130 nm LCK,Src,MEK1 A10095 A10100 A10109 AT9283 Aurora A Inhibitor I AZD1152-HQPA (Barasertib) J Biol Chem.291(45): AZD1152-HQPA (Barasertib) purchased from Adooq AZD 1152-HQPA is a highly potent and selective inhibitor of Aurora B, with Ki values to be 0.36 (Aurora B) and 1369 nm (Aurora A) respectively and has a high specificity versus a panel of 50 other kinases. Available package size: 5,10,50,100mg A10184 A10248 A10352 CCT CYC116 ENMD-2076 ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nm and 1.86 nm, 25- fold selective for Aurora A than over Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα. Phase 2. Available package size: 5,10,50,100mg PLoS One Apr 15;11(4):e Hesperadin purchased from Adooq Hesperadin is a human Aurora B inhibitor with an IC50 of 40 nm for the prevention of the phosphorylation of substrate. It markedly reduces the activity of AMPK, Lck, MKK1, MAPKAP-K1, CHK1 and PHK while it does not inhibit MKK1 activity in vivo. Available package size: 5,10,50,100mg A10494 A10508 A10601 A10714 A10715 A10851 A10981 JNJ KW-2449 MLN8054 PHA Danusertib (PHA ) SNS-314 VX-680 (MK-0457, Tozasertib) PNAS. 113(35): VX-680 purchased from Adooq VX-680 is a potent and selective small-molecule inhibitor of the Aurora kinases. Available package size: 25,50,100,250mg A11009 ZM A11066 AMG 900 A11067 TAK-901 A11081 CCT A11168 GSK A11171 PF A11410 MK-5108 (VX-689) A13069 XL-228 A13250 Reversine A13396 MK-8745 A13567 TC-A-2317 HCl A14059 SCH A14382 SAR A15011 AZD1152 A15762 BI A15970 HOI-07 Sirtuins A10377 A10388 A10862 EX 527 (Selisistat) Fisetin (Fustel) SRT1720 HCl Available package size: 5,10,50,200mg Journal of Neurochemistry, 2016, 140(6): SRT1720 HCl purchased from Adooq

8 7 Epigenetics Epigenetics 8 A12226 Sirtinol A12815 C646 A13806 JIB-04 A14226 Anacardic Acid A12527 Inauhzin A12948 UNC1215 A14267 MG149 A12904 A14188 AK-7 SRT2104 (GSK ) A13068 A13163 CPI-203 Bromosporine Sci Rep. 2017; 7: JIB-04 purchased from Adooq Histone Methyltransferase A14225 AGK2 A14370 AK-1 A15247 SRT 1720 A15902 SirReal2 Epigenetic Reader Domain The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do A13165 I-CBP112 A13227 SGC-CBP30 A13451 PF-4 A13717 UNC 669 A13749 MS436 A13890 OTX015 A13956 RVX-208 A13957 PFI-3 A14015 GSK2801 JIB-04 is a pan-selective Jumonji histone demethylase inhibitor with IC50 of 230, 340, 855, 445, 435, 1100, and 290 nm for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D, respectively. Available package size: 25,50,100mg A14277 IOX1 A14366 PBIT A14443 SP2509 (HCI-2509) A15547 GSK A11377 DZNep Oncotarget Dec 5; 8(63): DZNep purchased from Adooq 3 Deazaneplanocin A (DZNep) is a cyclopentenyl analog of 3-deazaadenosine, originally synthesized as an inhibitor of S-adenosyl-L-homocysteine hydrolase. Available package size: 1,2,5,10mg Inhibitor Name Epigenetic Reader Domain ()-JQ1 BRD4(2),IC50: 33 nm;brd4(1),ic50: 77 nm Bromosporine CECR2,IC50: 17 nm;brd2,ic50: 0.41 μm;brd9,ic50: μm;brd4,ic50: 0.29 μm CPI-203 BRD4,IC50: 37 nm GSK A BRD4,IC50: 22 nm;brd3,ic50: 31 nm;brd2,ic50: 41 nm I-BET151 BRD3,IC50: 0.25 μm;brd2,ic50: 0.5 μm;brd4,ic50: 0.79 μm A14133 A14134 A14160 A14226 A15367 GSK A GSK A (-)-JQ1 Anacardic Acid UNC 926 hydrochloride A15829 ML-324 A15893 ORY-1001 (RG-6016) A16177 CPI 4203 A16178 CPI 455 A16371 AS8351 A11599 A11757 UNC3866 GSK126 Oncotarget, 2015, 6(32), GSK126 purchased from Adooq I-BET-762 BET proteins,ic50: 35 nm A15872 I-BRD9 A ,4-Pyridinedicarboxylic Acid MS436 BRD4(1),Ki: <0.085 μm;brd4(2),ki: 0.34 μm OTX015 BRDs,EC50: nm PFI-1 BRD4,IC50: 0.22 μm PFI-3 RVX-208 BD2,IC50: 0.51 μm SGC-CBP30 CREBBP,IC50: 21 nm;ep300,ic50: 38 nm UNC1215 L3MBTL3-D274A,IC50: 3.5 μm;l3mbtl3,ic50: 40 nm;l3mbtl3,kd: 120 nm;l3mbtl3,ic50: 40 nm;l3mbtl3,kd: 120 nm UNC669 L3MBTL3,IC50: 35 μm;l3mbtl4,ic50: 69 μm;l3mbtl1,ic50: 6 μm;l3mbtl3,ic50: 35 μm A11440 A11783 GSK A (I-BET-762) GSK A (I-BET151) A15876 PF-CBP1 A15947 BAZ2-ICR A16000 OF-1 A16068 BI-7273 A16076 CPI 0610 A16092 GSK 5959 A16180 EML 425 A16196 BI-9564 A16330 GSK6853 A16355 CeMMEC13 A16373 TC-E 5002 A16374 CBB1007 DNA Methyltransferases A10005 A10105 A10292 (-)-Epigallocatechin gallate Azacitidine(Vidaza) Decitabine GSK126 is a potent, highly selective, S-adenosyl-methioninecompetitive, small-molecule inhibitor of EZH2 methyltransferase activity, decreases global H3K27me3 levels and reactivates silenced PRC2 target genes. Available package size: 2,5,10,25mg A11763 BIX A12439 EPZ A12585 MS023 A12711 EI1 A12712 EPZ-6438 (Tazemetostat) J. Biol Chem Dec 19; 289(51): GSK A (I-BET151) purchased from Adooq A16366 OXF BD 02 A16367 GW841819X A16368 BET-BAY 002 A16470 CPI-637 Mol Cell Proteomics Sep; 15(9): Decitabine purchased from Adooq Decitabine is a hypomethylating agent. It hypomethylates DNA by inhibiting DNA methyltransferase. A12735 EPZ-5676 (Pinometostat) A12812 Chaetocin A12929 MI-2 (Menin-MLL inhibitor 2) A12941 SGC 0946 GSK A is a novel selective inhibitor of the bromodomain and extra terminal (BET) family proteins BRD2, BRD3, and BRD4. Available package size: 5,10,25,50mg A12545 PFI-1 Histone Demethylases A12732 GSK-J4 PLoS One. 2015; 10(10): e GSK-J4 purchased from Adooq Available package size: 10,25,50,100mg A12744 SGI-110 (Guadecitabine) A12785 Lomeguatrib A13054 RG108 A13477 Nanaomycin A A13706 O6-Benzylguanine A14120 SGI 1027 A12947 UNC0638 A12983 EPZ A13061 AZ505 A13110 Opicapone (BIA ) A13114 GSK343 Sci Rep. 2017; 7: A14240 Procainamide HCl PFI-1 purchased from Adooq PFI-1 is a BET bromodomain inhibitor that exhibits inhibitory activity at BRD2 and BRD4. Available package size: 5,10,25,50mg A12704 A12729 SF1126 (+)-JQ1 (+)-JQ1 is a potent, high affinity, selective BET bromodomain inhibitor. Available package size: 5,10,25,50mg GSK J4 is a cell permeable prodrug rapidly hydrolyzed by macrophage esterases to GSK-J1, a potent selective jumonji H3K27 demethylase inhibitor; attenuates lipopolysaccharide (LPS)- induced proinflammatory cytokine production in primary human macrophages. Available package size: 10,25,50mg A12734 A12918 A12927 A13246 A13358 CBB1003 GSK J1 LSD1-C76 OG-L002 Tranylcypromine hydrochloride Histone Acetyltransferases A12814 Garcinol A12815 C646 A13378 NU 9056 A14215 Remodelin Nat Commun. 2017; 8: Remodelin purchased from Adooq Remodelin is a potent acetyl-transferase NAT10 inhibitor. Available package size: 10,25,50mg GSK343 is a potent histone H3-lysine 27 (H3K27) methyltransferase EZH2 inhibitor (IC= 4 nm). Diplays 1000-fold selectivity for other HMTs except EZH1 (60-fold selectivity). GSK343 inhibits H3K27 methylation in HCC1806 cells with an IC of <200nM. Available package size: 5,10,25,50mg A13166 UNC-1999 A13169 AZ505 ditrifluoroacetate A13194 UNC0646 A13195 UNC0631 A13200 UNC0321 A13282 UNC 2400 A13690 UNC 0638

9 9 Epigenetics Apoptosis 10 A13876 A13947 A14216 A14218 A14315 A14320 A14374 C deazaneplanocin A HCl (DZNep HCl) PFI-2 MI-3 MM-102 UNC0379 GSK591 Cell Rep Dec 19; 21(12) GSK591 purchased from Adooq GSK591 is a potent selective inhibitor of the arginine methyltransferase PRMT5 with IC50 of 11 nm. Available package size: 5,10,25mg A14401 BRD4770 A15388 UNC 0224 Bcl-2 Family Apoptosis A15450 SGC 707 A15487 UNC0642 A15544 EPZ A15549 GSK503 A15807 XY1 A15813 LLY-507 A15870 HLCL-61 A15908 CPI-360 A15916 AMI-1 A15920 CPI-169 A15928 WDR A15969 A-366 A16357 CPI-1205 A16375 EPZ A16377 EPZ A16378 TC-E 5003 A16405 Amodiaquine dihydrochloride dihydrate The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do A10665 Obatoclax mesylate (GX15-070) Int. J. Mol. Sci. 2017, 18(1), 44; Obatoclax purchased from Adooq Obatoclax mesylate (GX15-070) is Bcl-2 homology domain-3 (BH3) mimetic,antagonize all antiapoptotic Bcl-2 family proteins (average IC50, 3 umol/l), including Mcl-1 (IC50, 2.9 umol/l) and Bfl-1 (IC50, 5 umol/l). Available package size: 5,10,25,50mg A10955 A11448 A11988 A12500 A12743 A12823 TW-37 HA14-1 Gambogic acid ABT-199 (Venetoclax) BM-1074 Sabutoclax Oncotarget Jan 31; 8(5): Sabutoclax purchased from Adooq Sabutoclax(BI-97C1) is a pan-bcl-2 inhibitor, including Bcl-xL, Bcl-2, Mcl-1 and Bfl-1 with IC50 of 0.31 μm, 0.32 μm, 0.20 μm and 0.62 μm, respectively. Available package size: 5,10,25,50mg A12907 BAM 7 A13327 WEHI-539 hydrochloride A13578 AT101 acetic acid A13580 Bcl-2 Inhibitor A14222 UMI-77 A14795 Acetate gossypol A15004 AT-101 A15335 Bax channel blocker A15336 Bax inhibitor peptide P5 A15337 Bax inhibitor peptide V5 A15338 Bax inhibitor peptide, negative control A15340 Muristerone A A15545 A A15821 BDA-366 A16061 BH3I-1 A16112 A A16190 A A16192 CID A16314 Apogossypolone (ApoG2) A16315 MIM1 A16316 (+)-Apogossypol A16323 (S)-Gossypol acetic acid A16380 Pyridoclax Inhibitor Name Bcl-2 Bcl-B Bcl-w Bcl-xL Mcl-1 A1 Bax Other ABT-737 EC50: 30.3 nm EC50: 1.82 μm EC50: nm EC50: 78.7 nm Caspase Navitoclax (ABT-263) Ki: 1 nm Ki: 1 nm Ki: 0.5 nm Ki: 550 nm Ki: 354 nm Obatoclax Mesylate Ki: 0.22 μm TW-37 Ki: 0.29 μm Ki: 1.11 μm Ki: 0.26 μm Venetoclax Ki: <0.01 nm Ki: 245 nm Ki: 48 nm AT101 Ki: 0.32 μm Ki: 0.48 μm Ki: 0.18 μm HA14-1 IC50: 9 μm Sabutoclax IC50: 0.62 μm IC50: 0.31 μm IC50: 0.20 μm IC50: 0.62 μm A IC50: 26.2 nm UMI-77 Ki: 490 nm Gambogic Acid IC50: 1.21 μm IC50: 0.66 μm IC50: 0.02 μm IC50: 1.47 μm IC50: 0.79 μm IC50: 1.06 μm Caspase BM-1074 Ki: < 1 nm Ki: < 1 nm WEHI-539 HCl IC50: 1.1 nm BDA-366 Ki: 3.3 nm BH3I-1 Ki: 2.4 μm p53 A Ki: <0.01 nm A Ki: <0.01 nm Apogossypolone (ApoG2) A10022 ABT-263 (Navitoclax) A10255 ABT-737 The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name Pan- Caspase Caspase -1 Caspase -2 Caspase -3 Caspase- 4 Caspase -5 Caspase -6 Caspase -7 Caspase -8 Caspase -9 Caspase -10 VX-765 (Belnacasan) Z-VAD-FMK Z-DEVD- FMK Q-VD-OPh hydrate Caspase-3/7 Inhibitor I Z-VEID- FMK Z-VDVAD- FMK Z-DQMD- FMK Z-IETD- FMK Z-LEHD- FMK Z-FA- FMK Ivachtin Boc-D- FMK Z-WEHD- FMK Ac-DEVD- CHO IC50= mm Ki: 0.8 nm IC50: 50 nm Ki: 10 nm Ki: 1.71 μm IC50: 25 nm Ki: 60 nm IC50: 23 nm Ki: 230 pm Ki: <0.6 nm Ki: 132 nm Ki: 205 nm Ki: 31 nm Ki: 170 nm Ki: 1.6 nm IC50: 100 nm Ki: 0.92 nm IC50: 430 nm Ki: 60 nm Cancer Sci Sep; 107(9): Neoplasia Other ABT-263 purchased from Adooq ABT-263 (Navitoclax) is a potent orally bioavailable SMI that is structurally related to ABT-737. ABT-263 disrupts Bcl-2 - Bcl-XL interactions with pro-apoptotic proteins. Available package size: 5,10,25,100mg Apr;19(4): ABT-737 purchased from Adooq ABT-737 is a pan-bcl-2 inhibitor. IC50 values ranged from 192 nm (the pre-b cell line Hal-01) to <10 μm (Nalm-6, K562 and HL-60). Available package size: 5,10,50,100mg A10984 VX-765 (Belnacasan) VX-765 is a novel Caspase-1 inhibitor,which is an enzyme that controls the generation of two cytokines, IL-1b and IL-18. Available package size: 5,10,50,100mg PNAS Oct 28; 111(43): VX-765 purchased from Adooq

10 11 Apoptosis Apoptosis 12 A11090 PAC-1 A11944 Apoptosis Activator 2 p53 MDM2 A12373 Z-VAD-FMK Oncol Rep Jul; 38(1): Z-VAD-FMK purchased from Adooq Z-VAD-FMK is a cell-permeable, irreversible pan-caspase inhibitor. Inhibits caspase processing and apoptosis induction in tumor cells in vitro (IC50 = mm). Active in vivo. Available package size: 1,5,10,25mg A12611 Z-VEID-FMK A12637 Z-VDVAD-FMK A10491 JNJ A11523 RG7112 A11931 RITA (NSC ) A11943 Tenovin-1 A12305 Tenovin-6 A12449 Pifithrin-u A12450 Pifithrin-beta A12451 Pifithrin-alpha Exp Neurol Jul; 269: Pifithrin-alpha purchased from Adooq J Spinal Cord Med. 2015; 38(6) Necrostatin-1 purchased from Adooq Necrostatin-1 is an ATP-competitive, allosteric inhibitor of receptorinteracting protein kinase 1 (RIPK1) (EC50 = 182 nm). Available package size: 10,25,50mg A11974 GW 4869 A12748 QNZ (EVP4593) The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name Mdm2 Other Idasanutlin (RG-7388) IC50: 6 nm MI-773 (SAR405838) IC50: 0.88 nm p53 MX69 Kd: 2.34 μm Nutlin-3 IC50: 180 nm Nutlin-3a IC50: 90 nm Nutlin-3b IC50: 13.6 μm RG-7112 Kd: 11 nm YH239-EE A10657 Nutlin-3 A12697 A12800 A13070 Z-DQMD-FMK Z-IETD-FMK LY (Tasisulam) Science Apr 28;356(6336). LY purchased from Adooq LY is a potent anti-tumor agent, which causes growth arrest and apoptosis of a variety of human solid tumors in vitro and in vivo. LY induced apoptosis occurs by a mitochondrial-targeted mechanism. Available package size: 5,10,25,50mg A13503 Z-DEVD-FMK Scientific Reports, 2016, 6, Z-DEVD-FMK purchased from Adooq Z-DEVD-FMK is a specific, irreversible Caspase-3 inhibitor. Available package size: 2,5,25mg A hydroxy Cholesterol A14100 Nivocasan (GS-9450) A14284 Z-FA-FMK A14358 Z-LEHD-FMK A14915 Q-VD-OPh hydrate A14916 Z-WEHD-FMK A14919 Caspase-3/7 Inhibitor I A15291 Ac-LEHD-AFC A15294 AZ A15300 Ivachtin A15308 PETCM A15319 Ac-IEPD-AFC A15392 Boc-D-FMK A15816 Ac-DEVD-CHO A16317 Z-YVAD-FMK A16340 Z-VAD(OH)-FMK A16381 Z-FA-FMK Pifithrin-a is a reversible inhibitor of p53-mediated apoptosis and p53-dependent gene transcription such as cyclin G, p21/waf1, and mdm2 expression. Available package size: 5,10,25,50mg A12930 NSC A13117 NSC A13413 NSC59984 A13522 CP HCl A13581 PRIMA-1 A13636 APR-246 A13727 Tenovin-3 A13797 Kevetrin HCl A15201 p53 and MDM2 proteins-interaction-inhibitor chiral A15202 p53 and MDM2 proteins-interaction-inhibitor racemic A15346 CP dihydrochloride A15348 MIRA-1 A15349 NSC hydrochloride A15350 PhiKan 083 A15351 RETRA hydrochloride A15352 SJ A15353 WR 1065 TNF-alpha The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name TNF-α Other Pomalidomide IC50: 13 nm Necrostatin-1 EC50: 490 nm QNZ IC50: 7 nm NF-κB Thalidomide Lenalidomide (CC-5013) 13 nm A10522 A10743 A10924 A11973 Lenalidomide (CC-5013) Pomalidomide (CC-4047) Thalidomide Necrostatin-1 J Biol Chem Mar 1; 288(9) QNZ (EVP4593) purchased from Adooq QNZ inhibits the activation of the transcription factor NF-κB and has been used to investigate NF-κB signaling. Available package size: 5,10,25,50mg A15183 Necrostatin 2 A15327 Necrostatin 2 racemate A15328 Necrostatin 2 S enantiomer IAP The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name ciap XIAP Other AT406 (SM-406) ciap1-bir3, Ki: 1.9 nm; ciap2-bir3, Ki: 5.1 nm Birinapant Kd: <1 nm Kd: 45 nm BV-6 Embelin IC50: 4.1 μm 5-LO,mPGES-1 GDC-0152 Ki: 14.5 μm Ki: 28 nm MLXBIR3SG LCL161 SM-164 ciap1, IC50: 0.31 nm; ciap2, IC50: 1.1 nm A11163 A11928 IC50: 0.56 nm AT-406 (SM-406, ARRY ) LCL-161 Cell Res Jun; 25(6): LCL-161 purchased from Adooq LCL161 is an orally bioavailable second mitochondrial-derived activator of caspases (SMAC) mimetic and inhibitor of IAP (Inhibitor of Apoptosis Protein) family of proteins, with potential antineoplastic activity. Available package size: 5,10,25mg A12738 Birinapant (TL32711) A13055 Embelin A13058 Apoptosis Inhibitor (M50054) A14135 GDC-0152 A14231 BV-6 A15800 SM-164 Cell Cycle. 2016; 15(1): Nutlin-3 purchased from Adooq MDM2 antagonist nutlin-3 is a potent inducer of apoptosis. Available package size: 5,25,50,100mg A11179 A11501 NSC (XI-006) Nutlin 3a BMC Cancer. 2011; 11: 211. Nutlin 3a purchased from Adooq Nutlin 3a is a potent inhibitor of MDM2 (mouse double minute 2) binding to p53 that induces the expression of p53 regulated genes, and shows potent antiproliferative activity in cells expressing functional p53. Available package size: 5,10,25,50mg A11502 Nutlin 3b A11523 RG7112 A13582 MDM2 Inhibitor A13797 Kevetrin HCl A14051 WK23 A14118 YH239-EE A14211 Idasanutlin (RG7388) A14394 AMG232 A14423 MI-773 (SAR405838) A15201 p53 and MDM2 proteins-interaction-inhibitor chiral A15202 p53 and MDM2 proteins-interaction-inhibitor racemic A15352 SJ A15440 MI-773 A16326 NVP-CGM097 A16348 MX-69 PERK

11 13 Apoptosis PI3K / Akt / mtor 14 The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name PERK Other GSK IC50: 0.4 nm EIF2AK1 (HRI),EIF2AK2 (PKR) GSK IC50: 0.9 nm ISRIB (trans-isomer) IC50: 5 nm Salubrinal A12676 A12792 Survivin Salubrinal GSK Cell Death Dis Mar; 6(3): e1672. GSK purchased from Adooq GSK is an orally available, potent, and selective PERK inhibitor with IC50 of 0.4 nm. Available package size: 5,10,25,50mg A13577 A13816 A14302 A16075 A11002 GSK ISRIB (trans-isomer) ISRIB Azoramide YM155 (Sepantronium Bromide) Int J Oncol Sep; 47(3): YM155 purchased from Adooq YM155 is a novel small molecule survivin suppressant with an IC50 of 0.54 nm for the inhibition of survivin promoter activity. Available package size: 5,10,25,100mg A15284 Akt A10003 YM-155 HCl MK HCl RIP Kinase A11973 Necrostatin-1 A12615 GSK481 A16311 GSK583 A16312 RIP2 kinase inhibitor 1 A16313 RIP2 kinase inhibitor 2 ASK A12838 NQDI 1 A15991 Selonsertib c-ret The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name c-ret Other Danusertib IC50: 31 nm Aurora A,Abl,TrkA Regorafenib IC50: 1.5 nm Raf-1,VEGFR2,Kit RPI-1 IC50: 0.97 µm TG IC50: 17 nm JAK2,FLT3,JAK3 A10250 Regorafenib (BAY ) A10715 Danusertib (PHA ) A11180 TG A13832 RPI-1 A15218 Regorafenib monohydrate Protein kinase D (PKD) A12416 CID A12423 kb NB A13804 CID A13809 CID A16318 CRT PI3K / Akt / mtor Nature communications, 2016, 7, MK-2206 purchased from Adooq MK HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nm/12 nm/65 nm, respectively. Available package size: 5,10,25,50mg A10094 A10453 A10709 AT7867 Honokiol Perifosine (NSC ) Cell Death & Disease, 2017, 8(1), e2554. Perifosine (NSC ) purchased from Adooq Perifosine (also KRX-0401) acts as an Akt inhibitor and a PI3K inhibitor. Available package size: 5,10,50,200mg A11024 PF The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name Akt Akt1 Akt2 Akt3 Other 10-DEBC HCl IC50: 2.5 μm A Ki: 160 pm A Ki: 11 nm PKA,CDK2,GSK-3β Afuresertib Ki: 0.08 nm Ki: 2 nm Ki: 2.6 nm Akti-1/2 IC50: 58 nm IC50: 210 nm IC50: 2119 nm ARQ-092 (Miransertib) IC50: 5 nm IC50: 4.5 nm IC50: 16 nm AT13148 IC50: 38 nm IC50: 402 nm IC50: 50 nm PKA,ROCK2,ROCK1 AT7867 IC50: 32 nm IC50: 17 nm IC50: 47 nm PKA,p70 S6K AZD5363 IC50: 3 nm IC50: 8 nm IC50: 8 nm ROCK2 CCT IC50: 6 nm p70 S6K,PKA Deguelin PI3K GSK IC50: 2 nm IC50: 13 nm IC50: 9 nm PKCθ,PKCη,PrkX Honokiol MEK Ipatasertib IC50: 5 nm IC50: 18 nm IC50: 8 nm Miltefosine PI3K,PKC MK HCl IC50: 8 nm IC50: 12 nm IC50: 65 nm Perifosine IC50: 4.7 μm PF IC50: 3.8~7.5 nm PI3Kδ,PI3Kα,PI3Kγ PHT-427 Ki: 2.7 μm PDK-1 TIC10 ERK TIC10 Analogue ERK Triciribine IC50: 130 nm HIV-1 Uprosertib IC50: 180 nm IC50: 328 nm IC50: 38 nm A11030 GSK A11031 CCT A11032 PHT-427 A11033 Triciribine phosphate (NSC ) A11034 A Biochem Biophys Res Commun Apr 15;472(4): A purchased from Adooq A is a B/Akt inhibitor with an IC50 of 14 nm and also shows inhibitory activity against PKA and CDK2 with IC50 of 16 and 46 nm, respectively. Available package size: 5,10,25,50mg A11246 GDC-0068 (Ipatasertib, RG-7440) A11286 AKT inhibitor VIII (AKTI-1/2) A11287 A A11759 AZD5363 A12081 SC 66 A12435 Akt-l-1 A12464 AT13148 A12720 TIC10 isomer A12877 KP372-1 A13030 Afuresertib HCl A13210 Triciribine A13460 Deguelin A13554 SR A DEBC HCl A14138 Miltefosine A15006 AT7867 2HCl A15541 SC79 A15809 A15903 A16233 A16285 A16286 A16392 PI3K A10088 A10112 A10133 A10172 A10421 A10438 A10463 A10547 GSK (Uprosertib, GSK795) TIC10 Tomatidine Akt1 and Akt2-IN-1 ARQ-092 (Miransertib) Afuresertib AS AZD6482 BEZ235 (NVP-BEZ235, Dactolisib) CAL-101 (GS-1101, Idelalisib) GDC-0941 (Pictilisib) GSK IC LY Sci Rep. 2017; 7: LY purchased from Adooq LY is a PI3k inhibitor (cell IC50 about 10 μm) and a casein kinase II inhibitor. Available package size: 10,25,50,200mg A10726 A10727 A10728 A10729 A10730 PI-103 PIK-293 PIK-294 PIK-75 PIK-90

12 15 PI3K / Akt / mtor PI3K / Akt / mtor 16 The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name PI3K p110α p110β p110δ p110γ C2α C2β Vps34 Other Targets 3-Methyladenine IC50: 60 μm IC50: 25 μm A66 IC50: 32 nm IC50: 3.48 μm IC50: 462 nm PI4Kβ Acalisib Alpelisib IC50: 5 nm AMG319 IC50: 33 μm IC50: 2.7μM IC50: 18 nm IC50: 850 nm Apitolisib IC50: 5 nm IC50: 27 nm IC50: 7 nm IC50: 14 nm mtor AS IC50: 935 nm IC50: 33 nm Casein Kinase 2 AS IC50: 4.5 μm IC50: 0.25 μm AS IC50: 60 nm 270 nm IC50: 300 nm IC50: 8 nm AZD6482 IC50: 870 nm IC50: 10 nm IC50: 80 nm IC50: 1090 nm DNA-PK AZD8186 IC50: 35 nm IC50: 3 nm IC50: 17 nm IC50: 675 nm AZD8835 IC50: 6.2 nm IC50: 431 nm IC50: 5.7 nm IC50: 90 nm BGT226 IC50: 4 nm IC50: 63 nm IC50: 38 nm mtor Buparlisib IC50: 52nM IC50: 166nM IC50: 116nM IC50: 262nM IC50: 2.4 μm mtor CAL-130 CAY10505 CH IC50: 14 nm IC50: 0.12 μm IC50: 0.50 μm IC50: 36 nm CNX-1351 IC50: 6.8 nm Copanlisib IC50: nm IC50: 3.72 nm IC50: 0.7 nm IC50: 6.4 nm CUDC-907 IC50: 19 nm IC50: 54 nm IC50: 39 nm IC50: 311 nm HDAC1, HDAC3, HDAC10 CZC24832 IC50: 1.1 μm IC50: 8.2 μm IC50: 27 nm D IC50: <10 nm Dactolisib IC50: 4nM IC50: 75nM IC50: 7nM IC50: 5nM mtor (p70s6k), ATR Duvelisib Ki: pm Ki: 1564 pm Ki: 23 pm Ki: 243 pm ETP IC50: 2.3 nm IC50: 14.2 nm ETP IC50: 170 nm mtor, DNA-PK, ATR, ATM GDC-0084 Ki: 2 nm Ki: 46 nm Ki: 3 nm Ki: 10 nm mtor Gedatolisib IC50: 0.4 nm IC50: 5.4 nm mtor GNE-317 GNE-493 IC50: 3.4 nm IC50: 12 nm IC50: 16 nm IC50: 16 nm mtor GSK IC50: 0.4 nm IC50: 0.6 nm IC50: 2 nm IC50: 5 nm mtor GSK HS-173 IC50: 0.8 nm IC IC50: 75 μm IC50: 0.5 μm IC50: 29 μm Idelalisib IC50: 820nM IC50: 565 nm IC50: 2.5 nm IC50: 89 nm IC50: 978 nm DNA-PK IPI-549 IC50: 3.2 μm IC50: 3.5 μm IC50: 8.4 μm IC50: 16 nm LY IC50: 0.5μM IC50: 0.97μM IC50: 0.57 μm LY DNA-PK,mTOR kinase MLN1117 IC50: 15 nm NVP-BAG956 IC50: 56 nm IC50: 444 nm IC50: 34 nm IC50: 117 nm PDK1 NVP-QAV-572 Omipalisib Ki: nm Ki: 0.13 nm Ki: nm Ki: 0.06 nm mtorc1, mtorc2 ON IC50: 14 nm IC50: 20 nm Panulisib ALK1, mtor, DNA-PK PF Ki: 1.8 nm Ki: 2.1 nm Ki: 1.6 nm Ki: 1.9 nm P-Akt (S473), P-Akt (T308), mtor PF IC50: 9.1 nm Ki= 0.13 nm Ki=0.122 nm Ki=0.111 nm mtor PF IC50: 2 nm IC50: 142 nm IC50: 1 nm IC50: 65 nm PI-103 IC50: 2 nm IC50: 3 nm IC50: 3 nm IC50: 15 nm DNA-PK, mtor PI-3065 IC50: 2299 nm IC50: 1078 nm IC50: 15 nm IC50: nm Pictilisib (GDC-0941) IC50: 3nM IC50: 33nM IC50: 3nM IC50: 75 nm IC50: 0.67 μm mtor PIK-293 IC50: 100 μm IC50: 25 μm IC50: 0.24 μm IC50: 10 μm PIK-294 IC50: 490 nm IC50: 10 nm IC50: 160 nm PIK-75 HCl IC50: 5.8 nm IC50:0.51 μm IC50: 76nM DNA-PK PIK-90 IC50: 11 nm IC50: 350 nm IC50: 58 nm IC50: 18 nm PIK-93 IC50: 39 nm IC50: 590 nm IC50: 120 nm IC50: 16 nm IC50: 16 μm IC50: 140 nm IC50: 320 nm PI4KIIIδ, DNA-PK, ATM PIK-III IC50: 3.96μM IC50: 1.2μM IC50: 3.04μM IC50: 18nM Pilaralisib (XL147) IC50: 39 nm IC50: 36 nm IC50: 36 nm IC50: 23 nm PKI-402 IC50: 2 nm IC50: 7 nm IC50: 14 nm IC50: 16 nm mtor PQR309 PX-866 (Sonolisib) IC50: 5.5 nm IC50: 300 nm IC50: 2.7 nm IC50: 9.0 nm Quercetin IC50: 5.4 μm IC50: 3.0 μm IC50: 2.4 μm PKC, Src,S irtuin Taselisib (GDC 0032) Ki: 0.29 nm Ki: 9.1 nm Ki: 0.12 nm Ki: 0.97 nm IC50: 292 nm IC50: 374 nm TG IC50: 1.3 μm IC50: 1.2 μm IC50: 235 nm IC50: 83 nm TG IC50: 165 nm IC50: 215 nm IC50: 24 nm IC50: 50 nm TGR-1202 IC50: 22.2 nm TGX-221 IC50: 5 μm IC50: 5 nm IC50: 0.1 μm Voxtalisib IC50: 39 nm IC50: 113 nm IC50: 43 nm IC50: 9 nm DNA-PK,mTOR VPS34-IN1 IC50: 25 nm VS-5584 (SB2343) IC50: 2.6 nm IC50: 21 nm IC50: 2.7 nm IC50: 3.0 nm mtor Wortmannin IC50: 3 nm DNA-PK, ATM, MLCK XL147 analogue IC50: 39 nm IC50: 383 nm IC50: 36 nm IC50: 23 nm YM IC50: 3.3 μm PIKfyve ZSTK474 IC50: 37 nm IC50: 16 nm IC50: 44 nm IC50: 4.6 nm IC50: 49 nm A10731 PIK-93 Scientific reports, 2016, 6: PIK-93 purchased from Adooq PIK 93 selectively inhibits the type III PI 4-kinase enzyme, and small interfering RNA-mediated down-regulation of the individual PI 4-kinase enzymes. Available package size: 5,10,25,50mg A10765 A10766 A10922 A10923 A10995 A10997 A11014 A11016 Quercetin dihydrate (Sophoretin) Quercetin (Sophoretin) TG TGX-221 XL147 analogue XL765 ZSTK474 BKM120 (NVP-BKM120, Buparlisib) Clin Cancer Res Dec 1;19(23): BKM120 purchased from Adooq BKM120 (NVP-BKM120) is a bioavailable specific oral pan-class I phosphatidylinositol 3-kinase (PI3K) kinase inhibitor. Available package size: 5,10,25,50mg A11023 GDC-0980 (Apitolisib, RG7422) A11024 PF A11035 GSK (Omipalisib) A11064 YM A11079 PKI-587 ( Gedatolisib ) A11089 PKI-402 A11098 NU-7441 (KU-57788) A11099 AS A Methyladenine A11153 CUDC-907 A11161 Wortmannin Oncogene Mar; 36(11): Wortmannin purchased from Adooq Wortmannin is a potent, selective, cell-permeable and irreversible inhibitor of PI 3-kinase (IC50 = 2-4 nm) which also potently inhibits PLK1 (IC50 = 5.8 nm). Available package size: 5,10,25,50mg A11162 A11169 A11196 NVP-BGT226 CH CAY10505 A11197 AS A11198 D A11202 A66 A11261 PX-866 (Sonolisib) A11328 BYL719 (Alpelisib) A11363 CZC24832 A11511 NVP-BAG956 A11766 BAY (Copanlisib) A11784 GSK A11956 TG A12422 IPI-145 (Duvelisib, INK1197) A12480 VS-5584 A12704 SF1126 A12831 GDC-0032 (Taselisib) A12889 PF A12935 PF A13021 HS-173 A13328 ETP A13879 CNX-1351 A13992 GNE-317 A14109 PI3k-delta inhibitor 1 A14114 GNE 477 A14138 Miltefosine A14164 AZD8186 A14338 PI-3065 A14379 Panulisib (P7170, AK151761) A14432 GNE-493 A14441 Acalisib (GS-9820) A15030 CAL-130 A15031 CAL-130 Hydrochloride A15147 LY A15195 NVP-BKM120 Hydrochloride A15212 PI-103 Hydrochloride A15283 XL-147 (Pilaralisib) Int J Cancer Aug 1;139(3): XL-147 purchased from Adooq XL147 is a potent, orally bioavailable inhibitor of the class I PI3K family of lipid kinases. Available package size: 5,10,25mg A15430 PI4KIII beta inhibitor 3 A15529 MLN1117 (Serabelisib) A15759 AZD8186 A15868 PIK-III A15874 VPS34-IN1 A15901 AMG319 A15992 PQR309 A16126 LY A16266 ON A16269 PI4KIIIbeta-IN-10 A16270 PI4KIIIbeta-IN-9 A16271 ETP A16272 GDC-0084 A16273 NVP-QAV-572 A16274 PI3K-alpha inhibitor 1

13 17 PI3K / Akt / mtor PI3K / Akt / mtor 18 A16275 PI3K-gamma inhibitor 1 A16276 SAR (XL765, Voxtalisib) A16277 TGR-1202 mtor A16278 A16332 A16352 TGR-1202 hydrochloride IPI-549 AZD8835 The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name mtor mtorc1 mtorc2 Other Apitolisib Ki app: 17 nm p110α,p110δ,p110γ AZD8055 IC50: 0.8~0.13 nm DNA-PK,PI3Kδ,PI3Kα BGT226 PI3Kα,PI3Kγ,PI3Kβ CC-223 IC50: 16 nm cfms,flt4,dna-pk CH IC50: 1.6 μm PI3Kα,PI3Kγ,PI3Kβ Chrysophanic Acid EGFR Dactolisib IC50: 6 nm p110α,p110γ,p110δ ETP IC50: 0.6 nm ATR,DNA-PK,PI3Kα Everolimus IC50: 1.6 nm-2.4 nm GDC-0349 Ki: 3.8 nm PI3Kα Gedatolisib IC50: 1.6 nm PI3Kα,PI3Kγ GNE-493 IC50: 32 nm PI3Kα, PI3Kδ, PI3Kγ, PI3Kβ GSK IC50: 12 nm PI3Kα,PI3Kβ,PI3Kδ INK 128 Ki: 1.4 nm PI3Kα,PI3Kγ,PI3Kδ KU IC50: ~10 nm IC50: ~10 nm LY PI3Kα, Akt1, DNA-PK MHY1485 mtor inhibitor (mtor-in-1) Ki: 1.5 nm Omipalisib Ki: 0.18 nm Ki: 0.3 nm p110α,p110δ,p110γ OSI-027 IC50: 4 nm IC50: 22 nm IC50: 65 nm PI3Kγ,DNA-PK,PI3Kα Palomid 529 PF Ki: 16 nm PI3Kδ,PI3Kα,PI3Kγ PF IC50: 2.64 nm PI3Kα, PI3Kδ, PI3Kγ, PI3Kβ, Akt PI-103 IC50: 30 nm p110α,p110δ,p110β PP121 IC50: 13 nm PDGFR,Hck,VEGFR QL-IX-55 Rapamycin IC50: ~0.1 nm Ridaforolimus IC50: 0.2 nm SF1126 PI3K Tacrolimus Temsirolimus IC50: 1.76 μm Torin 1 IC50: 4.32 nm IC50: 2 nm IC50: 10 nm DNA-PK,p110γ,C2α Torin 2 IC50: 0.25 nm ATM,ATR,DNA-PK Torkinib IC50: 8 nm p110δ,pdgfr,dna-pk Vistusertib IC50: 2.8 nm P-Akt (S473),pS6 (S235/236) Voxtalisib IC50: 157 nm PI3Kγ,PI3Kα,PI3Kδ Voxtalisib Analogue IC50: 157 nm PI3Kγ,PI3Kα,PI3Kδ VS-5584 IC50: 3.4 nm PI3Kα, PI3Kδ, PI3Kγ, PI3Kβ WAY-600 IC50: 9 nm PI3Kα,PI3Kγ WYE IC50: 0.19 nm WYE-354 IC50: 5 nm PI3Kα,PI3Kγ WYE-687 IC50: 7 nm PI3Kα,PI3Kγ,p38α XL388 IC50: 9.9 nm IC50: 8 nm IC50: 166 nm CYP2C9,CYP3A4 Zotarolimus IC50: 2.8 nm A10114 AZD8055 A10133 BEZ235 (NVP-BEZ235, Dactolisib) A10295 Deforolimus (Ridaforolimus) A10374 BMC Developmental Biology Everolimus (RAD001) :42 AZD8055 purchased from Adooq A10389 A10438 FK-506 (Tacrolimus) GSK A10505 KU AZD8055 is a potent, selective, and orally bioavailable ATPcompetitive mtor kinase inhibitor with an IC50 of 0.8 nm. Available package size: 10,25,50,100mg A10693 A10726 Palomid 529 (P529) PI-103 A10746 A10782 PP242 (Torkinib) Rapamycin (Sirolimus) Journal of Diabetes Research, 2016, 2016: Rapamycin purchased from Adooq Rapamycin (Sirolimus) prevents activation of T cells and B-cells by inhibiting their response to interleukin-2 (IL-2). Available package size: 5,25,50,100mg A10906 A10989 Temsirolimus (Torisel) WYE-354 (Degrasyn) Oncotarget Oct 13; 6(31): WYE-354 purchased from Adooq WYE-354 is a potent cell-permeable inhibitor of mtor (IC50 = 4.3 nm) which blocks signaling through both mtor complex 1 (mtorc1) and mtorc2. It is a much weaker inhibitor of PI3K α (IC50 = 1026 nm) and other kinases. Available package size: 5,10,25,50mg A10997 XL765 A11023 GDC-0980 (Apitolisib, RG7422) A11024 PF A11035 GSK (Omipalisib) A11038 WYE (WYE-132) A11056 OSI-027 A11079 PKI-587 ( Gedatolisib ) A11162 NVP-BGT226 A11169 CH A11187 WYE-687 A11188 WAY-600 A11207 PP121 A11303 AZD2014 (Vistusertib) A11443 GDC-0349 A11461 INK 128 (MLN0128) A11537 QL-IX-55 A11586 Torin 2 A11587 Torin 1 Proc Natl Acad Sci USA Aug 30; 113(35): Torin 1 purchased from Adooq Torin1 is a potent inhibitor of mtor with IC50 of 2-10 nm. Available package size: 10,25,50,100mg A11950 Zotarolimus A12395 XL388 A12480 VS-5584 A12935 PF A13078 CC-223 A13328 ETP A13519 AP1903 A14114 GNE 477 A14432 GNE-493 A15147 LY A15175 mtor inhibitor (mtor-in-1) A15508 MHY1485 A15779 CC-115 A16126 LY A16276 SAR (XL765, Voxtalisib) PDK1 The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name PDK-1 Other BX-517 IC50: 6 nm BX-795 IC50: 6 nm TBK1/IKKɛ,c-Kit,CDK2/CyclinE BX-912 IC50: 12 nm PKA,KDR,CDK2/CyclinE GSK IC50: 10 nm NVP-BAG956 IC50: 240 nm PI3K OSU IC50: 5 μm PHT-427 Ki: 5.2 μm Akt PS 48 Kd: 10.3 μm A10681 A11032 A11148 OSU PHT-427 BX-795 Nat Commun. 2017; 8: 359. BX-795 purchased from Adooq BX-795 is a potent PDK1 inhibitor that blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induced apoptosis. Available package size: 10,25,50,100mg A11149 BX-912 A11511 NVP-BAG956 A11528 PDK1 inhibitor A12767 GSK A12881 BX-517 A13484 PS 48 Int J Biol Sci. 2017; 13(10): PS 48 purchased from Adooq PS 48 is an allosteric phosphoinositide-dependent protein kinase-1 (PDK1) activator (Kd = 10.3 μm). Available package size: 10,25,50,100mg A16185 A16279 PDK1 inhibitor TEPP-46

14 19 PI3K / Akt / mtor PI3K / Akt / mtor 20 DNA-PK The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name DNA-PK Other CC-115 IC50: 13 nm mtor Compound 401 IC50: 280 nm mtor,pi3k ETP IC50: 36 nm ATM, ATR, PI3Kα, mtor KU IC50: 8.6 nm PI3Kδ,PI3Kβ,PI3Kα NU7026 IC50: 0.23 μm PI3K NU7441 IC50: 14 nm mtor,pi3k PI-103 IC50: 23 nm p110α,p110δ,p110β PIK-75 IC50: 2 nm p110α,p110γ,p110δ PP121 IC50: 60 nm PDGFR,Hck,VEGFR A11423 FMK A11755 PF PF is a highly specific inhibitor of p70 ribosomal S6 kinase (S6K1) that inhibits S6K1-mediated phosphorylation of S6 protein in response to IGF-1, while having no effect on highly related RSK and MSK kinases. Available package size: 10,25,50,100mg A12452 BI-D1870 A10199 CHIR Stem Cell Reports Jan 9; 10(1): CHIR purchased from Adooq CHIR99021 is an aminopyrimidine derivative that inhibits GSK3α and GSK3β with IC50 values of 10 and 6.7 nm, respectively. Available package size: 2,5,25,100mg A10471 Indirubin A10825 SB A11061 SB A11085 CHIR The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name AMPK A EC50 = 0.8 μm Dorsomorphin Ki: 109 nm Dorsomorphin 2HCl Ki: 109 nm ETC-1002 HTH IC50: 100 nm WZ4003 IC50: 20 nm A11970 A13720 A14312 A15815 A15896 BML-275 (Dorsomorphin) Dorsomorphin 2HCl WZ4003 ETC-1002 GSK621 A10726 PI-103 A16281 HTH A10729 A11098 PIK-75 NU-7441 (KU-57788) Int J Biochem Cell Biol Blood Jan 15; 125(3): BI-D1870 purchased from Adooq Cancer Sci Jun; 108(6): CHIR purchased from Adooq A16282 A16283 A16284 Imeglimin Imeglimin hydrochloride YLF-466D Jun;87: NU-7441 purchased from Adooq NU-7441 (KU-57788) is a potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor. The IC50 values are 14, 1700, 5000, > and > nm for DNA-PK, mtor, PI 3-K, ATM and ATR respectively. Available package size: 5,10,50,100mg A11207 PP121 A11778 Compound 401 A12752 NU7026 A13224 KU A13328 ETP BI-D1870 is a potent and specific inhibitor of the p90 ribosomal S6 kinase (RSK) isoforms in vitro and in vivo, which inhibits RSK1, RSK2, RSK3 and RSK4 in vitro with an IC50 of nm. Available package size: 5,10,25,50mg A12464 A14202 A14372 A14373 A15006 A15527 AT13148 LY LJH685 LJI308 AT7867 2HCl LY tosylate salt CHIR is a very potent, selective, cell-permeable reversible inhibitor of GSK-3. Available package size: 5,10,50,100mg A11223 A11592 A11941 A12741 A12819 TWS119 Tideglusib TDZD-8 LY AZD1080 Oncotarget May 10; 7(19): AZD1080 purchased from Adooq MELK A12851 ATM / ATR OTSSP167 PNAS Aug 30; 113(35): OTSSP167 purchased from Adooq OTSSP167 is a highly potent MELK (maternal embryonic leucine zipper kinase) inhibitor with IC50 of 0.41 nm. Available package size: 5,10,25,50mg A14136 A15779 A16126 RSK The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name AT13148 AT7867 BI-D1870 FMK LJH685 LJI308 LY LY Tosylate PF SL p70 S6K p70 S6K1 RSK1 RSK2 RSK3 RSK4 IC50: 8nM IC50: 85nM IC50: 4nM IC50: 4nM NU6027 CC-115 LY IC50: 160nM A10094 AT7867 A11160 SL IC50: 85nM IC50: 31nM IC50: 24nM IC50: 18nM IC50: 15nM IC50: 15nM IC50: 6nM IC50: 5nM IC50: 4nM IC50: 6nM IC50: 4nM IC50: 13nM IC50: 89nM GSK-3 The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name GSK-3 GSK-3α GSK-3β Other 1-Azakenpaullone AR-A Ki: 38 nm AZD1080 IC50: 6.9 nm IC50: 31 nm AZD2858 IC50: 68 nm Bikinin BIO-acetoxime IC50: 10 nm IC50: 10 nm CHIR IC50: 0.65 nm IC50: 0.58 nm Cdc2 CHIR IC50: 10 nm IC50: 6.7 nm CP21R7 IM-12 IC50: 53 nm Indirubin IC50: 0.6 μm CDK5/p35, CDK2/CyclinA, CDK1/CyclinB Indirubin-3- monoxime IC50: 20 nm CDK1/5 LY IC50: 1.5 nm IC50: 0.9 nm SB IC50: 34.3 nm IC50: ~34.3 nm SB IC50: 78 nm IC50: ~78 nm TDZD-8 IC50: 2 μm Tideglusib IC50: 60 nm TWS119 IC50: 30 nm AZD1080 is a novel GSK3 inhibitor, rescues synaptic plasticity deficits in rodent brain and exhibits peripheral target engagement in humans. Available package size: 5,10,25,50mg A13060 AZD2858 A13728 AR-A A14196 IM-12 A Azakenpaullone A15471 GSK-3b A15526 Bikinin A15555 BIO-acetoxime A16230 CP21R7 A16280 Indirubin-3-monoxime AMPK A10028 Acadesine (Aicar,NSC ) A10717 Phenformin hydrochloride A11071 A Front Pharmacol. 2017; 8: 756. A purchased from Adooq Available package size: 5,10,50,100mg The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name ATM ATR Other AZ20 IC50: 5 nm mtor AZD6738 IC50: 1 nm CGK 733 IC50: 200 nm IC50: 200 nm CP IC50: 410 nm Dactolisib IC50: 21 nm p110α,p110γ,mtor (p70s6k) ETP IC50: 545 nm IC50: 14 nm mtor,dna-pk,pi3kα KU IC50: 12.9 nm DNA-PK,mTOR,PI3K KU IC50: 6.3 nm Schisandrin B IC50: 7.25 μm Torin 2 EC50: 28 nm EC50: 35 nm mtor,dna-pk VE-821 Ki: 13 nm VE-822 IC50: 34 μm IC50: 19 nm Wortmannin IC50: 150 nm IC50: 1.8 μm PI3K,DNA-PK,MLCK A10133 A10506 BEZ235 (NVP-BEZ235, Dactolisib) KU Int J Biochem Cell Biol Jun; 87: KU purchased from Adooq KU is an ATM inhibitor by suppressing cell proliferation and induces apoptosis by blocking Akt in cancer cells with overactivated Akt. Available package size: 5,10,50,100mg

15 Protein Tyrosine Kinases 21 PI3K / Akt / mtor 22 A10507 KU Oncology Letters, 2016, 12(1), KU purchased from Adooq KU is a potent and specific ATM inhibitor with IC50 of 6.3 nm. Available package size: 10,50,100mg A11086 CP A11161 Wortmannin A11586 Torin 2 A11605 VE-821 Virology Journal201613:15 VE-821 purchased from Adooq VE-821 is a potent and selective inhibitor of protein kinase ATR. Available package size: 10,25,50mg EGFR / HER2 A10005 A10043 A11991 Schisandrin B A13191 CGK 733 A13205 AZ-20 A13289 VE-822 A13328 ETP A14136 NU6027 A15794 AZD6738 Protein Tyrosine Kinases (-)-Epigallocatechin gallate AEE788 PLoS One. 2017; 12(6) e AEE788 purchased from Adooq AEE788 is an orally bioavailable multiple-receptor tyrosine kinase inhibitor that inhibits phosphorylation of the tyrosine kinases of EGFR, HER2 and VEGF2. Available package size: 5,10,25,50mg A10047 AG-490 A10053 Tyrphostin AG 879 A10062 AST-6 A10116 AZD8931 (Sapitinib) A10141 BIBW2992 (Afatinib) A10210 Chrysophanic acid (Chrysophanol) A10211 Canertinib (CI-1033) A10242 CP A10246 CUDC-101 A10286 Daphnetin A10362 Erlotinib HCl A10422 Gefitinib (Iressa) Available package size: 100,250,500mg Oncotarget Apr 18; 8(16) Gefitinib purchased from Adooq AZD6738 is a potent inhibitor of ATR kinase activity with an IC50 of 1 nm against the isolated enzyme and 74 nm against ATR kinasedependent CHK1 phosphorylation in cells. Available package size: 5,10,25mg A15842 A16419 A16445 A10426 Genistin (Genistoside) A10514 Lapatinib Ditosylate A10612 Mubritinib (TAK 165) A10638 Neratinib (HKI-272) A10678 OSI-420 A10702 PD (HCl salt) A10706 Pelitinib (EKB-569) A10990 WZ3146 A10991 WZ4002 A10992 WZ8040 A11022 AG-1478 (Tyrphostin AG-1478) Sci Rep. 2017; 7: AG-1478 purchased from Adooq AG-1478 is an inhibitor of EGFR kinase with an IC50 value of 3 nm. Available package size: 5,10,25,50mg A11027 A11028 Mirin AZD0156 Chloroquine Phosphate Arry-380 analog AV-412 Oncotarget Apr 12; 7(15): AV-412 purchased from Adooq AV-412 is an EGFR/HER2 inhibitor that binds to and inhibits the EGFR and HER2, which may result in the inhibition of tumor growth and angiogenesis. Available package size: 2,5,10,25mg The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name EGFR/ErbB1 HER2/ErbB2 ErbB3 ErbB4 Other AC480 IC50: 20 nm IC50: 30 nm IC50: 190 nm AEE788 IC50: 2 nm IC50: 6 nm IC50: 160 nm MEK,LCK,VEGFR2 Afatinib IC50: nm IC50: 14 nm Afatinib Dimaleate IC50: nm IC50: 14 nm AG-1478 IC50: 3 nm AG-18 IC50: 35 μm AG-490 IC50: 0.1 μm IC50: 13.5 μm JAK2 ARRY-380 (Irbinitinib) IC50: 8 nm AST-1306 IC50: nm IC50: 3.0 nm IC50: 0.8 nm AV-412 IC50: 43nM IC50: 282 nm AZ5104 IC50: <1 nm IC50: 7 nm AZD3759 IC50: 0.3 nm BIBX 1382 IC50: 3 nm IC50: 3.4 μm Butein mtor Canertinib IC50: 1.5 nm IC50: 9.0 nm CGP IC50: 0.3 μm Chrysophanic Acid CL IC50: 370 pm CNX-2006 IC50: <20 nm PDGFR CP IC50: 10 nm CUDC-101 IC50: 2.4 nm IC50: 15.7 nm Dacomitinib IC50: 6.0 nm IC50: 45.7 nm IC50: 73.7 nm Daphnetin IC50: 7.67 µm PKC, PKA Erlotinib HCl IC50: 2 nm Gefitinib IC50: nm Genistein Icotinib IC50: 5 nm MEK1,Aurora B,LCK Irbinitinib (ARRY-380, ONT-380) IC50: 8 nm Lapatinib IC50: 10.8 nm IC50: 9.2 nm IC50: 367 nm c-src Lapatinib Ditosylate IC50: 10.8 nm IC50: 9.2 nm IC50: 367 nm c-src Mubritinib (TAK 165) IC50: 6.0 nm Neratinib IC50: 92 nm IC50: 59 nm KDR,Src OSI-420 IC50: 2 nm Osimertinib IC50: nm BLK,ACK1,BRK PD HCl Ki: 5.2 pm Src,MEK/ERK,Raf PD IC50: 0.70 nm Pelitinib IC50: 38.5 nm IC50: μm c-abl,flt1,c-fms Poziotinib IC50: 3.2 nm IC50: 5.3 nm IC50: 23.5 nm Rociletinib Ki: nm Sapitinib IC50: 4 nm IC50: 3 nm HDAC,HDAC1,HDAC6 TAK-285 IC50: 23 nm IC50: 17 nm IC50: 260 nm Src,VEGFR,JAK3 Tyrphostin 9 IC50: 460 μm Tyrphostin AG 183 IC50: 800 nm Tyrphostin AG 879 IC50: 1.0 μm Trk Varlitinib IC50: 7 nm IC50: 2 nm WHI-P154 IC50: 4 nm WHI-P180 IC50: 4.0 μm Cdk2 WZ3146 IC50: 2-5 nm WZ4002 IC50: 2-8 nm IC50: 4 nm WZ8040 topo II A11051 PF (Dacomitinib, PF299) A11057 XL647 (Tesevatinib) A11155 AST-1306 A11158 ARRY (Varlitinib) A11209 BMS (AC480) A11236 TAK-285 A11263 BMS A11334 BIBX 1382 A11752 Lapatinib (free base) Sci Rep. 2016; 6: Lapatinib purchased from Adooq Lapatinib is a dual tyrosine kinase inhibitor which interrupts the HER2 growth receptor pathway. Available package size: 10,25,50,100mg

16 Protein Tyrosine Kinases Protein Tyrosine Kinases A11949 AG-17 A14049 WHI-P 154 A10080 AP24534 (Ponatinib) A12003 A12448 (-)-Gallocatechin Butein A14408 A14416 ASP8273 (Naquotinib) EGF816 (Nazartinib) A10137 A10162 Bibf1120 (Vargatef) Brivanib alaninate (BMS ) Cell Res Apr; 22(4): SU-5402 purchased from Adooq A12650 PKC 412 (Midostaurin) A14877 Epidermal Growth Factor Receptor Peptide ( ) A10198 Dovitinib Dilactic acid (TKI258 Dilactic acid) A12725 PD PLoS One. 2016; 11(11): e PD purchased from Adooq PD is a potent, cell-permeable, irreversible inhibitor of EGFR with IC50 value of 700 pm. Available package size: 5,10,50mg A12867 CGP A12868 ARRY-543 (Varlitinib, ASLAN001) A13028 CO-1686 (Rociletinib, AVL-301) A13044 Poziotinib A13146 CL (EKI-785) A13588 Tyrphostin AG 183 A13673 EGFR Inhibitor A13681 AZD-9291 (Osimertinib) A13718 Icotinib Hydrochloride A13755 CNX-2006 A13825 Icotinib FGFR A14953 Compound 56 A14985 Afatinib dimaleate A15081 Erlotinib mesylate A15093 Gefitinib hydrochloride A15272 Vandetanib trifluoroacetate A15457 D A15509 WHI-P180 A15516 AZ5104 A15531 BIBX1382 A15551 AZD3759 A15940 AG-18 (Tyrphostin 23) A15955 DM1-SMCC A16193 EAI045 A16253 Anlotinib A16254 PD PD is a very potent inhibitor of EGFR with IC50 of 0.08 nm; pan-specific antagonist of ErbB receptor. Available package size: 5,50mg A16361 A16413 TX ARRY-380 (Irbinitinib) A10254 A10508 A10699 A10703 PD is a potent, cell permeable and ATP competitive inhibitor of FGFR and VEGFR. Available package size: 5,10,50,100mg A10715 A10953 Brain, 2015, 138(4), TSU-68 purchased from Adooq TSU-68 (SU-6668) is an inhibitor of RTKs involved in VEGF, bfgf and PDGF signaling, which inhibits endothelial cell proliferation. Available package size: 5,10,50,100mg A11075 Brivanib (BMS ) KW-2449 Pazopanib HCl (GW786034) PD Danusertib (PHA ) TSU-68 (Orantinib, SU6668) AZD4547 J Biol Chem Oct 26; 287(44): PD purchased from Adooq SU-5402 is a potent and selective vascular endothelial growth factor receptor (VEGFR) and fibroblast growth factor receptor (FGFR) inhibitor (IC50 values are 0.02, 0.03, 0.51 and > 100 μm at VEGFR2, FGFR1, PDGFRβ and EGFR respectively). Available package size: 5,10,25,50mg A11753 MK-2461 A12357 FIIN-2 A13069 XL-228 A13111 R1530 A13211 SSR128129E A14415 Debio-1347 (CH ) A14431 ACTB-1003 A15073 E-3810 A15194 NVP-BGJ398 phosphate A15534 BLU9931 A15848 FIIN-3 A15946 Alofanib (RPT835) A15957 Erdafitinib (JNJ ) A16197 Nintedanib esylate A16251 FGFR4-IN-1 A16252 H3B-6527 PDGFR The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name FGFR FGFR1 FGFR2 FGFR3 FGFR4 Other Alofanib (RPT835) AZD4547 IC50: 0.2 nm IC50: 2.5 nm IC50: 1.8 nm IC50: 165 nm KDR,IGFR BGJ398 IC50: 0.9 nm IC50: 1.4 nm IC50: 1.0 nm IC50: 60 nm VEGFR2,Lyn,Kit BLU9931 IC50: 591 nm IC50: 493 nm IC50: 150 nm IC50: 3 nm Brivanib IC50: 148 nm VEGFR2,Flk1,VEGFR1 Brivanib Alaninate IC50: 148 nm VEGFR2,Flk1,VEGFR1 CH IC50: 9.3 nm IC50: 7.6 nm IC50: 22 nm IC50: 290 nm VEGFR2 Danusertib IC50: 47 nm Aurora A,Abl,TrkA Dovitinib IC50: 8 nm IC50: 9 nm FLT3,c-Kit,VEGFR3/FLT4 Dovitinib Dilactic Acid IC50: 8 nm IC50: 9 nm FLT3,c-Kit,VEGFR3/FLT4 E-3810 IC50: 17.5 nm IC50: 82.5 nm VEGFR1, VEGFR2, VEGFR3 Erdafitinib FIIN-2 IC50: 3.09 nm IC50: 4.3 nm IC50: 27 nm IC50: 45.3 nm FLT3,c-Kit,VEGFR3/FLT4 FIIN-3 IC50: 13 nm IC50: 21 nm IC50: 31 nm IC50: 35 nm KW-2449 IC50: 36 nm FLT3, Bcr-Abl, Aurora A, PDGFRβ, IGF-1R, EGFR LY IC50: 2.8 nm IC50: 2.6 nm IC50: 6.4 nm IC50: 6 nm MK-2461 IC50: 65 nm IC50: 39 nm IC50: 50 nm Nintedanib IC50: 69 nm IC50: 37 nm IC50: 108 nm IC50: 610 nm VEGFR3,VEGFR2,LCK Orantinib Ki: 1.2 μm PDGFRβ,Flk1 Pazopanib 74 nm VEGFR1, VEGFR2, VEGFR3, PDGFR, c-kit, c-fms Pazopanib HCl 74 nm VEGFR1, VEGFR2, VEGFR3, PDGFR, c-kit, c-fms PD IC50: ~25 nm VEGFR2,c-Src Ponatinib IC50: 2.2 nm Abl,PDGFRα,VEGFR2 R 1530 Kd: μm Chk2, KDR, FGFR, Aurora A, Cdk2, VEGFR-2, PDGFRβ SSR128129E IC50: 1.9 μm VEGFR2,PDGFRβ SU5402 IC50: 30 nm Oncotarget Apr 12; 7(15): AZD4547 purchased from Adooq AZD4547 is a potent, selective and orally active pan-fgfr inhibitor, with IC50s of 0.2, 2.5, 1.8 and 165 nm for FGFR1, 2, 3 and 4, respectively. Available package size: 5,10,50,100mg A11159 BGJ398 (NVP-BGJ398) Proc Natl Acad Sci USA Nov 11; 111(45): E4869 E4877. BGJ398 purchased from Adooq BGJ398 is a potent and selective inhibitor with potential antiangiogenic and antineoplastic activities of fibroblast growth factor receptor (FGFR) tyrosine kinases 1, 2, 3 and 4 (with IC50 values of 0.9, 1.4, 1.0 and 60 nm for FGFR1, FGFR2, FGFR3, and FGFR4 respectively). Available package size: 5,10,50,100mg A11244 LY A11411 Dovitinib (TKI-258) A11518 Pazopanib (GW ) A11558 SU-5402 A10001 A10025 A10080 Sorafenib (Nexavar) Linifanib (ABT-869) AP24534 (Ponatinib) PLoS One. 2013; 8(10) e AP24534 purchased from Adooq AP24534 (Ponatinib) is a potent multi-kinase and pan-bcr-abl inhibitor. Available package size: 10,25,50,100mg A10101 Tivozanib (AV-951) A10103 Axitinib A10137 Bibf1120 (Vargatef) A10198 Dovitinib Dilactic acid (TKI258 Dilactic acid) A10250 Regorafenib (BAY ) A10259 Imatinib (Gleevec) A10468 Imatinib Mesylate A10502 Ki8751 A10504 KRN 633 A10558 Masitinib (AB1010) A10608 Motesanib Diphosphate (AMG-706) A10610 MP470 (MP-470, Amuvatinib) A10699 Pazopanib HCl (GW786034) A10880 Sunitinib Malate

17 Protein Tyrosine Kinases Protein Tyrosine Kinases The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name PDGFR PDGFRα PDGFRβ Other Amuvatinib IC50: 40 nm c-kit (D816H),FLT3 (D835Y) Axitinib IC50: 5.0 nm IC50: 1.6 nm VEGFR1/FLT1,VEGFR2/Flk1,VEGFR3 AZD2932 IC50: 4 nm Flt3,VEGFR-2,c-Kit CP IC50: 10 nm IC50: 1 nm c-kit,vegfr2,vegfr1 Crenolanib Kd: 2.1 nm Kd: 3.2 nm DCC-2618 IC50: 30 nm IC50: 13 nm c-kit Dovitinib IC50: 210 nm IC50: 27 nm FLT3,c-Kit,FGFR1 Dovitinib Dilactic Acid IC50: 210 nm IC50: 27 nm FLT3,c-Kit,VEGFR3/FLT4 Imatinib IC50: 100 nm c-kit,v-abl Imatinib Mesylate c-kit,v-abl Ki8751 IC50: 67 nm VEGFR2,c-Kit,FGFR2 KRN 633 IC50: 965 nm IC50: 9850 nm VEGFR3,VEGFR2,VEGFR1 Linifanib IC50: 66 nm VEGFR1/FLT1,CSF-1R,FLT3 Masitinib IC50: 540 nm IC50: 800 nm Kit,Lyn B,Abl1 MK-2461 IC50: 22 nm c-met (M1250T),c-Met (Y1235D),c-Met (Y1230H) Motesanib Diphosphate IC50: 84 nm VEGFR1,VEGFR2,VEGFR3 Nintedanib IC50: 59 nm IC50: 65 nm VEGFR3,VEGFR2,LCK Orantinib Ki: 8 nm FGFR1,Flk1 Pazopanib IC50: 84 nm VEGFR1,VEGFR2,VEGFR3 Pazopanib HCl IC50: 84 nm VEGFR1,VEGFR2,VEGFR3 Ponatinib IC50: 1.1 nm Abl,VEGFR2,FGFR1 PP121 IC50: 2 nm Hck,VEGFR,mTOR Sorafenib Tosylate IC50: 100 nm IC50: 57 nm Raf-1,VEGFR2/Flk1,B-Raf Sunitinib Malate IC50: 2 nm FLT3,Kit,VEGFR2 Telatinib IC50: 15 nm c-kit,vegfr3,vegfr2 Tivozanib IC50: 40 nm IC50: 49 nm VEGFR2,VEGFR3,EphB2 A10903 Telatinib (BAY ) A10953 TSU-68 (Orantinib, SU6668) A11052 Crenolanib (CP ) A11207 PP121 A11350 CP A11472 Ki A11518 Pazopanib (GW ) Oncotarget Jan 10; 8(2): Pazopanib (GW ) purchased from Adooq Pazopanib is a potent and selective multi-targeted receptor tyrosine kinase inhibitor of VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-a/β, and c-kit that blocks tumor growth and inhibits angiogenesis. Available package size: 25,50,100mg A11581 Toceranib (PHA , SU 11654) A11753 MK-2461 A13111 R1530 A13530 Flumatinib mesylate A13545 JI-101 A13555 TAK-593 A14156 AZD 2932 A15062 DCC-2618 A15152 Masitinib mesylate A15182 N-Desethyl Sunitinib A15263 Toceranib phosphate A15933 AC710 A16197 A16246 A16258 VEGFR A10001 A10025 A10043 A10101 A10103 Nintedanib esylate AC710 Mesylate Flumatinib Sorafenib (Nexavar) Linifanib (ABT-869) AEE788 Tivozanib (AV-951) Axitinib Axitinib is a small molecule tyrosine kinase inhibitor,which inhibits multiple targets, including VEGFR-1, VEGFR-2, VEGFR-3, platelet derived growth factor receptor (PDGFR), and ckit (CD117). Available package size: 50,100,250mg A10137 Bibf1120 (Vargatef) A10154 BMS A10162 Brivanib alaninate (BMS ) A10185 Cediranib (AZD2171) A10198 Dovitinib Dilactic acid (TKI258 Dilactic acid) A10248 CYC116 A10250 Regorafenib (BAY ) A10254 Brivanib (BMS ) The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name VEGFR1 VEGFR2 VEGFR3 Other AEE788 IC50: 59 nm IC50: 77 nm IC50: 330 nm EGFR,HER2/ErbB2,c-Abl Apatinib IC50: 1 nm RET,c-Kit,c-Src Axitinib IC50: 0.1 nm IC50: nm IC50: nm PDGFRβ,Kit,PDGFRα AZD2932 IC50: 8 nm PDGFRβ,Flt3,c-Kit BAW2881 (NVP-BAW2881) hvegfr1, IC50: 820 nm hvegfr2, IC50: 9 nm; mvegf2, IC50: 165 nm hvegfr3, IC50: 420 nm C-Raf-1,B-RAFV599E,c-Abl BFH772 IC50: 3 nm BMS IC50: 15 nm Met BMS IC50: 15 nm c-met Brivanib IC50: 380 nm IC50: 25 nm FGFR1 Brivanib Alaninate IC50: 380 nm IC50: 25 nm FGFR1 Cabozantinib IC50: 12 nm IC50: nm IC50: 6.0 nm c-met,kit,axl Cediranib IC50: 5 nm IC50: 0.5 nm IC50: 3 nm c-kit,pdgfrβ,fgfr1 CP IC50: 11 nm FGFR CYC116 Ki: 44 nm Aurora A,Aurora B,FLT3 Dovitinib IC50: 10 nm IC50: 13 nm IC50: 8 nm FLT3,c-Kit,FGFR1 Dovitinib Dilactic Acid IC50: 10 nm IC50: 13 nm IC50: 8 nm FLT3,c-Kit,FGFR1 E-3810 IC50: 7 nm IC50: 25 nm IC50: 10 nm FGFR-1, FGFR-2 ENMD-2076 IC50: 58.2 nm IC50: 15.9 nm FLT3,RET,Aurora A Foretinib IC50: 6.8 nm IC50: 0.86 nm IC50: 2.8 nm Met,Tie-2,RON Golvatinib IC50: 16 nm c-met Ki8751 IC50: 0.9 nm c-kit,pdgfrα,fgfr2 KRN 633 IC50: 170 nm IC50: 160 nm IC50: 125 nm PDGFRα,c-Kit,BTK Lenvatinib IC50: 22 nm IC50: 4.0 nm IC50: 5.2 nm PDGFRβ,FGFR1,PDGFRα Linifanib IC50: 3 nm IC50: 4 nm IC50: 190 nm CSF-1R,FLT3,Kit ltiratinib (DCC2701) IC50: 9.2 nm MET, TIE2, TRK LY IC50: 7 nm FGFR2,FGFR1,FGFR4 MGCD-265 IC50: 3 nm IC50: 3 nm IC50: 4 nm Met,RON,Tie-2 Motesanib Diphosphate IC50: 2 nm IC50: 3-6 nm IC50: 6 nm Kit,RET,PDGFR Nintedanib IC50: 34 nm IC50: 13 nm IC50: 13 nm LCK,FLT3,FGFR2 Orantinib Ki: 2.1 μm PDGFRβ,FGFR1 OSI-930 IC50: 8 nm IC50: 9 nm CSF-1R,LCK,C-Raf Pazopanib IC50: 10 nm IC50: 30 nm IC50: 47 nm FGFR,PDGFR,c-Kit Pazopanib HCl IC50: 10 nm IC50: 30 nm IC50: 47 nm FGFR,PDGFR,c-Kit PD IC50: nm FGFR1,c-Src Ponatinib IC50: 1.5 nm Abl,PDGFRα,FGFR1 RAF265 EC50: 30 nm B-Raf Regorafenib IC50: 13 nm IC50: 4.2 nm IC50: 46 nm RET,Raf-1,Kit SAR IC50: 23 nm Semaxanib IC50: 1.23 μm SKLB1002 IC50: 32 nm SKLB610 IC50: 2.2 μm PDGFR, FGFR2 Sorafenib Tosylate IC50: 90 nm Raf-1,B-Raf,B-Raf (V599E) SU5402 IC50: 20 nm FGFR1,PDGFRβ Sunitinib Malate IC50: 80 nm Kit,FLT3,PDGFRβ Taxifolin (Dihydroquercetin) A10340 E7080 (Lenvatinib) Telatinib IC50: 6 nm IC50: 4 nm c-kit,pdgfrα TG IC50: 2 nm IC50: 7 nm FGFR1, Fyn, Src TG IC50: 2 nm IC50: 7 nm FGFR1, Fyn, Src Tivozanib IC50: 30 nm IC50: 6.5 nm IC50: 15 nm EphB2,PDGFRα,PDGFRβ Vandetanib IC50: 40 nm IC50: 110 nm Vatalanib 2HCl IC50: 77 nm IC50: nm IC50: 660 nm PDGFRβ,c-Kit,c-Fms ZM IC50: 0.33 μm Src,Abl ZM HCl IC50: <2 nm ZM IC50: 2 nm E7080 is a multi-kinase inhibitor that inhibits both VEGFR2 and VEGFR3 kinases. Available package size: 5,10,50,100mg A10352 ENMD-2076 A10502 Ki8751 A10504 KRN 633 A10587 MGCD-265 (Glesatinib) A10608 Motesanib Diphosphate (AMG-706)

18 Protein Tyrosine Kinases Protein Tyrosine Kinases A10679 A10699 A10703 A10773 OSI-930 Pazopanib HCl (GW786034) PD RAF265 (CHIR-265) A12437 A12693 A13111 A13234 SU 5416 (Semaxinib) NVP-BAW2881 R1530 SKLB1002 Onco Targets Ther. 2015; 8: BMS purchased from Adooq The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name FLT3 Other AMG 925 IC50: 1 nm CDK4,CDK1 A10774 A10880 A10893 Raf265 derivative Sunitinib Malate Taxifolin A10903 Telatinib (BAY ) A10963 Vandetanib (ZD6474) A13240 A13377 A13465 A13545 A13555 NVP-ACC789 SAR SKLB610 JI-101 TAK-593 A11059 A11175 BMS GSK A Amuvatinib IC50: 81 nm c-kit (D816H),PDGFRα (V561D) AST 487 Ki: 0.52 µm Ret, c-kit, KDR, c-abl AZD2932 PDGFRβ,VEGFR-2,c-Kit BPR1J-097 IC50: 11±7 nm Cabozantinib IC50: 11.3 nm VEGFR2/KDR,c-Met,Kit Dovitinib IC50: 1 nm c-kit,vegfr3/flt4,fgfr1 A10967 A10996 A10998 A11057 A11207 Vatalanib (PTK787) 2HCl XL184 free base (Cabozantinib) Foretinib (GSK , XL880) XL647 (Tesevatinib) PP121 A11244 LY A11263 A11396 A11407 A11411 BMS A11472 Ki A11496 E-7050 (Golvatinib) Apatinib (YN968D1) Apatinib (YN968D1) is a tyrosine kinase inhibitor that selectively inhibits the vascular endothelial growth factor receptor-2 (VEGFR2, also known as KDR) that inhibits VEGF-mediated endothelial cell migration and proliferation thus blocking new blood vessel formation in tumor tissue. Available package size: 5,10,50,100mg Dovitinib (TKI-258) Motesanib (AMG706) A13819 TG A13820 TG A14156 AZD 2932 A14387 Altiratinib (DCC2701) A14393 Fruquintinib A15073 E-3810 A15182 N-Desethyl Sunitinib A15218 Regorafenib monohydrate A15250 SU14813 double bond Z A15260 TG HCl A15261 TG HCl A15263 Toceranib phosphate A15271 Vandetanib HCl A15272 Vandetanib trifluoroacetate A15287 ZM A15760 SU10944 A15792 BMS A16197 Nintedanib esylate A16237 EG00229 A16342 BFH772 IGF-1R The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name IGF-1R Insulin Receptor Other AG-1024 IC50: 7 μm IC50: 57 μm Pflugers Arch Apr;468(4): GSK A purchased from Adooq GSK A is a small-molecule kinase inhibitor that inhibits IGF-IR and the insulin receptor with IC50s of 2.0 and 1.6 nmol/l, respectively. Available package size: 5,10,50,100mg A11400 AG-1024 (Tyrphostin) Mol Nutr Food Res Jun;58(6): AG-1024 purchased from Adooq AG-1024 (Tyrphostin) is a specific inhibitor of insulin-like growth factor-1 (IGF-1) and insulin receptor tyrosine kinase activity. Exhibits lower IC50 values for IGF-1 than for the insulin receptor. Also inhibits insulin-stimulated cellular proliferation. Available package size: 5,10,25,50mg A11951 PQ 401 A12195 Picropodophyllin A13069 XL-228 A16247 NT157 Dovitinib Dilactic Acid IC50: 1 nm c-kit,fgfr1,vegfr3/flt4 ENMD-2076 IC50: 1.86 nm RET,Aurora A,VEGFR3/FLT4 ENMD-2076 L-()-Tartaric acid RET,Aurora A,VEGFR3/FLT4 G-749 IC50: nm Mer,Aurora B,RET Gilteritinib (ASP2215) IC50: 0.29 nm Axl Go6976 JAK2,PKCα,PKCβ1 KW-2449 FLT3, IC50: 6.6 nm; FLT3 (D835Y), IC50: 1 nm Abl (T315I),Abl,FGFR1 Pacritinib IC50: 6-22 nm JAK2 (V617F),JAK2,TYK2 Pexidartinib (PLX3397) IC50: 160 nm Kit, CSF-1R Quizartinib IC50: nm R406 Syk SU5614 Tandutinib IC50: 0.22 μm c-kit,pdgfrβ,csf-1r TCS 359 IC50: 42 nm TG-02 (SB1317) IC50: 56 nm CDK2, JAK2 TG IC50: 25 nm JAK2,RET,JAK3 UNC2025 IC50: 0.8 nm Mer A10770 A10887 R406 (Tamatinib) Tandutinib (MLN518) Tandutinib (MLN518) inhibits the autophosphorylation of FLT3, c-kit and PDGF receptor tyrosine kinases, thereby inhibiting cellular proliferation and inducing apoptosis. Available package size: 25,50,100,200mg Mol Cancer. 2012; 11: 70. Motesanib purchased from Adooq Motesanib (AMG706) is a multikinase inhibitor that selectively targets VEGF receptors, platelet-derived growth factor receptors (PDGFRs), and Kit receptors with IC50 values of 2 nm (VEGFR1), 3 nm (VEGFR2), 6 nm (VEGFR3), 84 nm (PDGFR), and 8 nm (Kit). Available package size: 5,10,25,50mg A11518 A11557 A11558 Pazopanib (GW ) SU14813 SU-5402 A11581 Toceranib (PHA , SU 11654) A11737 A11772 A11954 A11955 A12027 Buflomedil HCl CP ZM hydrochloride ZM hydrochloride (-)-Catechin gallate BMS IC50: 100 nm IC50: 73 nm FAK,MEK,LCK BMS IC50: 1.8 nm IC50: 1.7 nm TrkB,Met,TrkA GSK A IC50: 2 nm IC50: 1.6 nm ALK,RSK1,JNK3 GSK A IC50: 27 nm IC50: 25 nm IKK3,VEGFR2,Syk Linsitinib IC50: 35 nm IC50: 75 nm IRR NVP-ADW742 IC50: 0.17 μm NVP-AEW541 IC50: 0.15 μm IC50: 0.14 μm FLT3,Tek,FLT1 Picropodophyllin IC50: 1 nm PQ 401 IC50: <1 μm A10440 A10658 A11021 A11053 A11054 GSK A NVP-ADW742 NVP-AEW541 OSI-906 BMS BMS is an effective inhibitor of IGF-IR, causing a reversion of an IGF-IR - mediated transformed phenotype. Available package size: 5,10,50,100mg FLT3 A10027 AC220 (Quizartinib) Mol Cancer Ther Feb;14(2): AC220 purchased from Adooq AC220 (Quizartinib) is a uniquely potent and selective FLT3 inhibitor with IC50 of 0.56 ± 0.3 nm and >10 mm for MC4-11 and A375, respectively. Available package size: 5,10,50,200mg A10198 A10352 A10508 A10610 A10769 Dovitinib Dilactic acid (TKI258 Dilactic acid) ENMD-2076 KW-2449 MP470 (MP-470, Amuvatinib) R406 besylate A10996 XL184 free base (Cabozantinib) A11180 TG A11411 Dovitinib (TKI-258) A11753 MK-2461 A11962 TG-02 (SB1317) A12419 Go 6976 A12427 TCS 359 A12694 Pacritinib (SB1518) A14025 AMG-925 A14156 AZD 2932 A14214 G-749 A14411 Gilteritinib (ASP2215) A15003 AST 487 A15520 Pexidartinib (PLX3397) A15548 SU5614 A15904 UNC-2025 A16246 AC710 Mesylate

19 Protein Tyrosine Kinases Protein Tyrosine Kinases A16248 A16249 A16250 c-met The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name c-met Other Altiratinib IC50: 2.7 nm TIE-2, VEGFR AMG-208 IC50: 9 nm AMG-458 Ki: nm VEGFR2 BMS IC50: 5.6 nm Insulin Receptor,IGF-1R,TrkB BMS IC50: 3.9 nm Axl,RON,Tyro3 BMS IC50: 1.7 nm VEGFR2 BMS IC50: 1.7 nm VEGFR2 Cabozantinib IC50: 1.3 nm VEGFR2/KDR,Kit,VEGFR3/FLT4 Capmatinib IC50: 0.13 nm Crizotinib IC50: 11 nm ALK Foretinib IC50: 0.4 nm KDR,Tie-2,VEGFR3/FLT4 Golvatinib IC50: 14 nm VEGFR2 JNJ IC50: 4 nm Merestinib Ki: 2 nm MGCD-265 IC50: 1 nm RON,VEGFR2,VEGFR1 MK-2461 IC50: nm c-met (Y1235D),c-Met (Y1230C),c- Met (N1100) MK-8033 IC50: 1 nm Ron NPS-1034 IC50: 48 nm Axl NVP-BVU972 IC50: 14 nm PF IC50: 4.8 nm PHA IC50: 9 nm RON,Flk1,c-Abl SGX-523 IC50: 4 nm SU11274 IC50: 0.01 μm Flk1,RON,FGFR1 Tepotinib IC50: 4 nm IRAK4,TrkA,Axl Tivantinib Ki: μm Volitinib BPR1J-097 FLT3-IN-1 FLT3-IN-2 A10063 AMG 208 A10153 BMS BMS is a MET tyrosine kinase inhibitor that binds to c-met protein, or HGFR, preventing binding of HGF and disrupting the MET signaling pathway. Available package size: 5,10,50,100mg A10154 A10493 A10587 A10711 A10712 A10713 A10839 A10869 A10996 A10998 BMS JNJ MGCD-265 (Glesatinib) PF PF (Crizotinib) PHA SGX-523 SU11274 XL184 free base (Cabozantinib) Foretinib (GSK , XL880) Clin Cancer Res Jan 1;21(1): Foretinib purchased from Adooq Foretinib (GSK ), a multikinase inhibitor of c-met and VEGFR-2, blocks proliferation, induces Anoikis, and impairs ovarian cancer metastasis. Available package size: 5,25,50,100mg A11055 AMG-458 A11059 BMS A11087 ARQ 197 A11132 INCB28060 A11150 NVP-BVU972 A11257 EMD A11396 E-7050 (Golvatinib) A11489 MK-8033 A11753 MK-2461 A12557 LY (Merestinib) A14387 Altiratinib (DCC2701) A14419 Volitinib (Savolitinib, AZD-6094) A15049 c-met inhibitor 1 A15150 LY dihydrochloride A15208 PF methanesulfonate A15792 BMS A15917 NPS-1034 A16256 c-met inhibitor 2 A16257 Glesatinib hydrochloride A16400 AMG 337 ALK The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name ALK Other Alectinib IC50: nm INSR,KDR AP26113 IC50: 0.62 nm FER,ROS/ROS1,FLT3 ASP3026 IC50: 3.5 nm AZD3463 Ki: 0.75 nm Brigatinib (AP26113) ALK, IC50: 0.37 nm; ROS1, IC50: 1.9 nm FLT3,IGF1R,EGFR(C797S/del19) CEP IC50 = 1.9 nm CEP IC50 = 120 nm FAK Ceritinib IC50: 0.2 nm Insulin Receptor,IGF-1R,STK22D Crizotinib IC50: 24 nm c-met Entrectinib TrkC,TrkB,TrkA GSK A IC50: 0.5 nm Insulin Receptor,IGF-1R,RSK1 HG IC50 = 20 nm KRCA-0008 IC50 = 12 nm Ack1 PF Ki: <0.07 nm LTK (TYK1),FER,FES (FPS) TAE684 IC50: 3 nm A10662 TAE684 TAE684 is a inhibitor of ALK and also a potent inhibitor of LRRK2 kinase activity (IC(50) of 7.8nM against wild-type LRRK2, 6.1nM against the G2019S mutant). Available package size: 5,10,50,100mg A10712 A11134 A11175 PF (Crizotinib) CH GSK A Eur J Physiol (2016) 468: GSK A purchased from Adooq GSK A is a small-molecule kinase inhibitor that inhibits IGF-IR and the insulin receptor with IC50s of 2.0 and 1.6 nmol/l, respectively. Available package size: 5,25,50,100mg A11773 A11948 SRC ASP3026 ALK-IN-1 (Brigatinib analog, AP26113 analog) A13065 AZD3463 A13238 LDK-378 A13450 Brigatinib (AP26113) A13744 CEP A14207 PF A14987 ALK inhibitor 1 A14988 ALK inhibitor 2 A15142 LDK378 dihydrochloride A15511 KRCA-0008 A15543 CEP A15801 Entrectinib A16245 Crizotinib hydrochloride A16267 HG The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name Src Lck Fyn Lyn Yes Other 1-NA-PP1 IC50: 1.0 nm IC50: 0.6 nm c-abl, CDK2, CAMK II A IC50: 147 nm AZM IC50: 5.0 nm Bosutinib IC50: 1.2 nm Abl Dasatinib IC50: 0.8 nm Abl,c-Kit (D816V),c-Kit (wt) Dasatinib Monohydrate IC50: 0.8 nm Abl,c-Kit (D816V),c-Kit (wt) KX2-391 GI50: 9 nm MCB-613 IC50: 9 nm IC50: <3 nm IC50: <3 nm MLR 1023 EC50: 63 nm NVP-BHG712 IC50: μm EphB4,C-Raf,c-Abl PD FGFR1, PDGFRβ, Wee1 PP1 IC50: 6 nm IC50: 5 nm IC50: 6 nm Kit,EGFR,Bcr-Abl PP2 IC50: 5 nm IC50: 4 nm IC50: 5 nm EGFR Quercetin Sirtuin,PKC,PI3Kγ Saracatinib IC50: 5 nm IC50: <4 nm IC50: 10 nm IC50: 5 nm EGFR (L861Q),c-YES,EGFR (L858R) SU6656 IC50: 130 nm IC50: 170 nm IC50: 130 nm IC50: 20 nm TG IC50: 1.0 nm IC50: 0.5 nm VEGFR1, VEGFR2, FGFR1 TG IC50: 1.0 nm IC50: 0.5 nm VEGFR1, VEGFR2, FGFR1 WH IC50: 6 nm IC50: 2 nm A10108 A10161 A10290 A10661 A10766 A11177 Saracatinib (AZD0530) Bosutinib (SKI-606) Dasatinib (BMS ) NVP-BHG712 Quercetin (Sophoretin) KX2-391 KX2-391 is a novel non-atp competitive substrate-pocket directed SRC inhibitor. Available package size: 5,10,50,100mg A11207 PP121 A11288 A A11471 KX HCl A12214 KX1-004 A12234 Scutellarein A12417 MLR 1023 A12723 PP2 PP2 is a selective inhibitor of Src-family tyrosine kinases. Inhibits p56lck and p59fynt (IC50 values are 4 and 5 nm respectively). Displays > fold selectivity over ZAP-70 and JAK2. Moderately inhibits CSK (IC50 = 0.73 μm). Available package size: 10,25,50,100mg A12724 PP1 A13069 XL-228 A13167 AMG-47a A NA-PP1 A13290 A A13415 MCB-613

20 Protein Tyrosine Kinases Protein Tyrosine Kinases A13573 PP1 Analog II, 1NM-PP1 A10198 Dovitinib Dilactic acid (TKI258 Dilactic acid) A10996 XL184 free base (Cabozantinib) A ,8-Dihydroxyflavone A13819 TG A10250 Regorafenib (BAY ) A13456 AMG-Tie2-1 A16238 GW A13820 TG A10259 Imatinib (Gleevec) A14387 Altiratinib (DCC2701) A16239 LOXO-101 sulfate TG is VEGFR2 and Src kinase inhibitor. Available package size: 5,10,25mg A13821 CGP77675 A13868 PD A14117 WH A14323 A A15060 Dasatinib hydrochloride A15140 Lck Inhibitor A15141 Lck inhibitor 2 A15260 TG HCl A15518 SU6656 A16086 Tilfrinib A16240 MNS A16241 AZM A16242 CPDA A16243 T338C Src-IN-1 A16244 T338C Src-IN-2 A16265 Lyn-IN-1 c-kit The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name c-kit Other Amuvatinib IC50: 10 nm PDGFRα (V561D),FLT3 (D835Y) Axitinib IC50: 1.7 nm VEGFR1/FLT1,VEGFR2/Flk1, VEGFR2/ KDR AZD2932 IC50: 9 nm PDGFRβ,Flt3,VEGFR-2 Cabozantinib IC50: 4.6 nm VEGFR2/KDR,c-Met,VEGFR3/FLT4 Dasatinib IC50: nm Abl,Src Dasatinib Monohydrate IC50: nm Abl,Src DCC-2618 IC50: 6 nm PDGFRα, PDGFRβ Dovitinib IC50: 2 nm FLT3,FGFR1,VEGFR3/FLT4 Dovitinib Dilactic Acid IC50: 2 nm FLT3,FGFR1,VEGFR3/FLT4 Imatinib Mesylate IC50: 100 nm PDGFR,v-Abl Ki8751 IC50: 40 nm VEGFR2,PDGFRα,FGFR2 Masitinib IC50: 200 nm Lyn B,PDGFRα,PDGFRβ Motesanib Diphosphate IC50: 8 nm VEGFR1,VEGFR2,VEGFR2/Flk1 OSI-930 IC50: 80 nm FLT1,KDR,CSF-1R Pazopanib IC50: 140 nm VEGFR1,VEGFR2,VEGFR3 Pazopanib HCl IC50: 140 nm VEGFR1,VEGFR2,VEGFR3 Pexidartinib (PLX3397) IC50: 10 nm CSF-1R, Flt-3 PLX647 IC50: 16 nm Fms Sunitinib Malate FLT3,PDGFRβ,VEGFR2 Telatinib IC50: 1 nm VEGFR3,VEGFR2,PDGFRα Tivozanib IC50: 78 nm VEGFR2,VEGFR3,EphB2 Vatalanib 2HCl IC50: 730 nm VEGFR2/KDR,VEGFR1/FLT1,VEGFR2/Flk1 A10101 A10103 Tivozanib (AV-951) Axitinib A10290 A10468 A10502 A10558 A10608 A10610 A10679 OSI-930 is a potent inhibitor of Kit, KDR, Flt, CSF-1R, c-raf and Lck with IC50 of 80 nm, 9 nm, 8 nm, 15 nm, 41 nm and 22 nm, respectively. Available package size: 5,25,50,100mg Tie-2 A10587 A10895 A10932 Dasatinib (BMS ) Imatinib Mesylate Ki8751 Masitinib (AB1010) Motesanib Diphosphate (AMG-706) MP470 (MP-470, Amuvatinib) OSI-930 A10699 Pazopanib HCl (GW786034) A10880 Sunitinib Malate A10903 Telatinib (BAY ) A10967 Vatalanib (PTK787) 2HCl A10996 XL184 free base (Cabozantinib) A11411 Dovitinib (TKI-258) A11472 Ki A11518 Pazopanib (GW ) A11581 Toceranib (PHA , SU 11654) A13530 Flumatinib mesylate A14156 AZD 2932 A15003 AST 487 A15062 DCC-2618 A15152 Masitinib mesylate A15182 N-Desethyl Sunitinib A15218 Regorafenib monohydrate A15519 PLX647 A15520 Pexidartinib (PLX3397) A16258 Flumatinib A16320 Dasatinib Monohydrate The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name Tie-2 Other Altiratinib (DCC2701) AMG-Tie2-1 IC50: <1 nm Cabozantinib IC50: 14.3 nm VEGFR2/KDR,c-Met,Kit MGCD-265 IC50: 7 nm Met,RON,VEGFR2 Pexmetinib (ARRY-614) p38 MAPK Tie2 kinase inhibitor IC50: 0.25 μm MGCD-265 (Glesatinib) Pexmetinib (ARRY-614) Tie2 kinase inhibitor Tyrosine kinase A13587 AG-1288 A13589 AG 957 A15267 Tyrosine kinase inhibitor Trk Receptors The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name TrkA TrkB TrkC 7,8-Dihydroxyflavone ANA-12 Kd: 10 nm BMS IC50: 7.4 nm IC50: 4.1 nm Danusertib (PHA ) Entrectinib (RXDX-101) GNF-5837 GW Larotrectinib (LOXO-101) sulfate LM22A-4 Sitravatinib (MGCD516) Tyrphostin AG 879 IC50: 31 nm Trk receptor Other Targets Insulin Receptor, IGF-1R,Met Aurora A, Abl, RET, FGFR1, Aurora C, Aurora B ALK,ROS1 IC50: 8 nm IC50: 12 nm IC50: 7 nm IC50: 2 nm IC50: 5 nm IC50: 10 μm IC50: 47 nm IC50: 9 nm A10053 Tyrphostin AG 879 A10715 Danusertib (PHA ) A11059 BMS A12666 AZ 23 A13730 GNF 5837 DDR2, EPHA3, Axl Her2 Int J Pharm Dec 30;515(1-2): GNF 5837 purchased from Adooq GNF-5837 is a potent, selective, and orally bioavailable pan-trk inhibitor that inhibited tumor growth in a mouse xenograft model derived from RIE cells expressing both TRKA and NGF. Available package size: 10,25,50,100mg A13877 ANA-12 ANA-12 is a TrkB receptor antagonist that demonstrates a 2-site mode of action, preventing activation by BDNF non-competitively. Available package size: 10,25,50mg A15345 TLQP 21 A15494 LM22A-4 A15801 Entrectinib A15974 LOXO-101 (ARRY-470, Larotrectinib) A16259 CSF-1R Sitravatinib The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name CSF-1R Other BLZ945 IC50: 1 nm CEP Kd: 9 nm c-kit,ret,pdgfrβ GW2580 IC50: 30 nm Ki IC50: 2 nm VEGFR-2, PDGFRβ, c-kit Linifanib IC50: 3 nm VEGFR1/FLT1,FLT3,VEGFR2/KDR OSI-930 IC50: 15 nm FLT1,KDR,LCK Pexidartinib IC50: 20 nm A10025 Linifanib (ABT-869) A10679 OSI-930 A11472 Ki J Bone Miner Res May; 32(5) Ki purchased from Adooq Ki is an inhibitor of c-fms tyrosine kinase (M-CSFR, CSF1R). Available package size: 10,25,50mg A11518 A11959 A12687 A13772 A15520 A15540 TAM Receptor Pazopanib (GW ) GW2580 JNJ CEP Pexidartinib (PLX3397) BLZ945 The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name Mer Axl Tyro3 Other BMS IC50: 14 nm IC50: 1.1 nm IC50: 4.3 nm KDR,c- VEGFR2/ Met,Kit Cabozantinib IC50: 7.0 nm LDC1267 IC50: <5 nm IC50: 29 nm IC50: 8 nm Met NPS-1034 IC50: 10.3 nm R428 IC50: 14 nm RON, Met, FLT3 TP-0903 IC50: 27 nm FLT3 UNC2025 IC50: 0.74 nm IC50: 14 nm IC50: 17 nm UNC2250 IC50: 1.7 nm IC50: 100 nm KDR,c- VEGFR2/ Met,Kit UNC2881 IC50: 4.3 nm IC50: 360 nm IC50: 250 nm A10153 BMS A10996 XL184 free base (Cabozantinib) A13003 LDC1267 A13741 R428 A13805 UNC569 A14143 UNC 2250 A14276 UNC2881

21 Protein Tyrosine Kinases 33 Angiogenesis 34 A14411 A15776 Gilteritinib (ASP2215) TP-0903 Ephrin Receptor A15358 A15359 Chetomin KC7F2 A12535 A12706 RN486 GDC-0834 TP-0903 is a potent and selective Axl kinase inhibitor with IC50 of 27 nm. Available package size: 5,10,25mg A12493 ALW-II A15360 ML 228 A15530 FG-2216 A15793 JNJ A15895 DASA-58 A13202 AVL-292 A16181 HIF-2a Translation Inhibitor A15864 A15917 A16257 SGI-7079 EGFR / HER2 NPS-1034 Glesatinib hydrochloride Detailed product information is on Page 21. FGFR Detailed product information is on Page 23. PDGFR Detailed product information is on Page 24. VEGFR Detailed product information is on Page 25. VDA The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name VDA Other Targets DMXAA (ASA404, Vadimezan) DT-diaphorase, Ki: 20 μm NPI-2358 (Plinabulin) Tubulin, IC50: 9.8 nm-18 nm Verteporfin YAP/TEAD interaction A10324 DMXAA (ASA404, Vadimezan) A10654 NPI-2358 (Plinabulin) A12658 Verteporfin A14352 Oxi 4503 Angiogenesis Cell Rep Sep 25; 8(6): DMXAA purchased from Adooq DMXAA (ASA404) is a tumorvascular disrupting agent (tumor- VDA) that attacks the blood supply of a cancerous tumor to cause tumor regression. Available package size: 5,25,50,100mg ALW-II is a novel Eph receptor tyrosine kinase inhibitor. Available package size: 5,10,50mg HIF The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name HIF HIF1 Other 2-Methoxyestradiol Microtubule Associated BAY FG-2216 IC50: 3.9 μm IC50: 3.9 μm KC7F2 IC50: 20 μm IC50: 20 μm PX-478 2HCl Roxadustat A10012 A Methoxyestradiol FG-4592 (Roxadustat) Proc Natl Acad Sci U S A May 3; 113(18): E2516 E2525. FG-4592 purchased from Adooq FG-4592 is a novel hypoxia inducible factor prolyl hydroxylase inhibitor, in CKD anemia. Available package size: 10,25,50,100mg A11924 IOX 2 PLoS One. 2015; 10(7): e IOX2 purchased from Adooq IOX2 is a potent inhibitor of HIF-1α prolyl hydroxylase-2 (PHD2) with IC50 of 21 nm in a cell-free assay, >100-fold selectivity over JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH. Available package size: 10,25,50mg A12671 GSK (Daprodustat) A12883 FM19G11 A12921 HIF-C2 A12978 BAY A14021 Echinomycin A14319 PX-478 HCl A14367 Oroxylin A A14404 Molidustat FLT3 Detailed product information is on Page 28. ALK Detailed product information is on Page 29. BTK The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name BTK Other ACP-196 (Acalabrutinib) IC50: 3 nm AVL-292 IC50: <0.5 nm YES,c-Src,BRK AVL-292 benzenesulfonate IC50: <0.5 nm YES,c-Src,BRK CGI1746 IC50: 1.9 nm CNX-774 IC50: <1 nm GDC-0834 IC50: nm Ibrutinib IC50: 0.5 nm BLK,Bmx,FGR LFM-A13 IC50: 2.5 μm Olmutinib (HM71224) IC50: 1.95 nm ONO-4059 analogue IC50: 23.9 nm PCI IC50: 8.2 nm QL47 IC50: 7 nm RN486 IC50: 4 nm A11020 PCI (Ibrutinib) PCI is an orally bioavailable small-molecule inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity. Available package size: 5,10,25,100mg A11348 CGI1746 CGI1746 is a small-molecule Btk inhibitor chemotype with a new binding mode that stabilizes an inactive nonphosphorylated enzyme conformation. Available package size: 2,5,10,25mg AVL-292 is a highly selective, covalent Btk inhibitor. Available package size: 5,10,25,50mg A13233 CNX-774 A15008 AVL-292 benzenesulfonate A15558 ONO-4059 A15824 ACP-196 (Acalabrutinib) A15976 Olmutinib (HM71224) A16260 Btk inhibitor 1 A16261 LFM-A13 A16262 PCI A16263 QL47 A16339 GDC0853 FAK The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name FAK Other CEP IC50: 2.3 nm ALK Defactinib GSK IC50: 0.4 nm PF IC50: 1.5 nm CDK2/CyclinE,CDK3/CyclinE,CDK1/CyclinB PF IC50: 22 nm Aurora A,Aurora B,FLT1 PF IC50: 2 nm PF IC50: 1.5 nm CDK2/CyclinE,CDK3/CyclinE,CDK1/CyclinB PF IC50: 4 nm PND-1186 IC50: 0.5 nm TAE226 IC50: 5.5 nm Insulin Receptor,IGF-1R,c-Met A11142 PF A11171 PF A11192 PF Nat Commun. 2016; 7: PF purchased from Adooq PF is an orally bioavailable small molecule and ATPcompetitive focal adhesion kinase (FAK) inhibitor with potential antineoplastic and antiangiogenic activities. Available package size: 5,10,50,100mg A11235 PF Sci Rep. 2016; 6: PF purchased from Adooq PF is a potent and selective inhibitor of focal adhesion kinase (FAK) (IC50 = 4 nm). Available package size: 10,25,50,100mg

22 35 Angiogenesis Angiogenesis 36 A11507 NVP-TAE 226 A11926 R788 (Fostamatinib) A10108 Saracatinib (AZD0530) A10715 Danusertib (PHA ) A11929 PF (Defactinib) A11952 P (PRT062607, BIIB057) A10988 WP1130 ( Degrasyn ) A12162 Piceatannol Cancer Sci May; Oncotarget Sep; 5(17): A12731 A13884 PRT HCL GS (5): Saracatinib purchased from Adooq PF purchased from Adooq PF is a novel FAK kinase inhibitor that decreases growth and induces apoptosis in pancreatic neuroendocrine tumor cells. Available package size: 2,5,10,25mg A12580 PF A13140 PND-1186 A13461 PF A15543 CEP A15765 GSK Syk The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name Syk Other BAY Ki: 7.5 nm Entospletinib IC50: 7.7 nm Fostamatinib IC50: 41 nm Adenosine A3 receptor, Adenosine transporter, Monoamine transporter MNS IC50: 2.5 μm p97, Src P IC50: 1 nm FGR, MLK1 Piceatannol Lyn, PKA, PKC PRT IC50: 4nM PRT HCl IC50: 1 nm FGR, MLK1, YES R112 IC50: 226 nm R406 (Tamatinib) IC50: 41 nm Flt3 R406 besylate IC50: 41 nm Flt3 R788 Disodium IC50: 41 nm A10769 A10770 R406 besylate R406 (Tamatinib) GS-9973 is an oral inhibitor of spleen tyrosine kinase (Syk), with potential antineoplastic activity. Available package size: 10,25,50,100mg A14161 A15017 A15524 A16240 BCR-ABL R112 BAY dihydrochloride PRT MNS The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name Bcr-Abl Abl Other AT9283 IC50: 4-30 nm JAK3,JAK2,Aurora B Bafetinib IC50: 5.8 nm IC50: 5.8 nm Lyn Danusertib IC50: 25 nm IC50: 25 nm Aurora A,TrkA,RET Dasatinib IC50: 0.6 nm IC50: 0.6 nm Src,c-Kit (D816V), c-kit (wt) Dasatinib Monohydrate IC50: 0.6 nm IC50: 0.6 nm Src,c-Kit (D816V), c-kit (wt) Degrasyn IC50: 1.8 μm DUB DPH Flumatinib mesylate IC50: 1.2 nm PDGFRβ, c-kit GNF-2 IC50: 273 nm GNF-5 IC50: 220 nm GNF-7 IC50: 122 nm IC50: 133 nm GZD824 Dimesylate IC50: 0.34 nm IC50: nm Imatinib Mesylate IC50: 600 nm c-kit,pdgfr KW-2449 IC50: 14 nm IC50: 4-14 nm FLT3 (D835Y), FLT3,FGFR1 Nilotinib IC50: <30 nm Saracatinib (AZD0530) is a highly selective, orally available, dualspecific Src/Abl kinase inhibitor with IC50 of 2.7 and 30 nm for c-src and Abl kinase, respectively. Available package size: 10,25,100,200mg A10119 Bafetinib (INNO-406) Nat Commun Apr 3;8: Bafetinib purchased from Adooq Bafetinib ((INNO-406) is a dual Bcr-Abl/Lyn tyrosine kinase inhibitor for the potential treatment of leukemia. Available package size: 5,10,50,100mg A10259 A10290 A10468 A10508 A10644 Imatinib (Gleevec) Dasatinib (BMS ) Imatinib Mesylate KW-2449 Nilotinib (AMN-107) Stem Cell Reports Oct 13; 5(4): Nilotinib (AMN-107) purchased from Adooq Nilotinib is a Bcr-Abl inhibitor with IC50 less than 30 nm. Available package size: 100,200mg A10661 NVP-BHG712 MAPK WP1130 (Degrasyn) is a novel selective small molecular deubiquitinase inhibitor and a Bcr/Abl destruction pathway activator that specifically and rapidly down-regulates both wild-type and mutant Bcr/Abl protein without affecting bcr/abl gene expression in chronic myelogenous leukemia (CML) cells. Available package size: 5,10,50,100mg A11200 DCC-2036 (Rebastinib) A11207 PP121 A11379 DPH A11439 GNF 2 A13029 Radotinib (IY-5511) A13069 XL-228 A13120 PD A13237 GNF-5 A13530 Flumatinib mesylate A13562 NRC-AN-019 A15003 AST 487 A15186 Nilotinib monohydrochloride monohydrate A15849 GZD824 Dimesylate A15887 GNF-7 A16258 Flumatinib A16264 GZD824 A16265 Lyn-IN-1 A16266 ON A16320 Dasatinib Monohydrate R406 is a potent inhibitor of immunoglobulin E (IgE)- and IgGmediated activation of Fc receptor signaling. Available package size: 10,25,50,100mg A10771 R (Fostamatinib disodium, R788) NVP-BHG712 IC50: μm EphB4,C-Raf,c-Src PD IC50: 1-2 nm Src AP24534 (Ponatinib) IC50: 0.37 nm IC50: 0.37 nm PDGFRα, VEGFR2, FGFR1 Radotinib IC50: 34 nm Rebastinib IC50: nm FLT3,KDR,Tie-2 Saracatinib IC50: 30 nm c-src, LCK, EGFR (L861Q) A10080 AP24534 (Ponatinib) MEK A10089 AS (Pimasertib) A10115 AZD8330 A10150 BIX02188 A10151 BIX A10256 A10257 PD AZD6244 (Selumetinib) Oncotarget Jun 7; 7(23): AZD6244 purchased from Adooq A11320 BAY PLoS One. 2013; 8(10): e AP24534 (Ponatinib) purchased from Adooq FEBS Open Bio Mar; 7(3): BIX purchased from Adooq AZD6244 (Selumetinib) also known as Selumetinib, ARRY142886, AZD-6244 & ARRY is MEK 1/2 inhibitor with GI50 values ranging from 14 to 50 nm. Available package size: 100,250,500mg BAY is a cell-permeable imidazopyrimidine compound that acts as a potent, ATP-competitive, reversible, and highly selective inhibitor of Syk tyrosine kinase activity with no inhibitory effect against Btk, Fyn, Itk, Lyn, and Src. Available package size: 5,10,25,50mg AP24534 (Ponatinib) is a potent multi-kinase and pan-bcr-abl inhibitor. Available package size: 10,25,50,100mg A10095 AT9283 BIX is a selective dual MEK5 and ERK5 (or BMK1) kinase inhibitor, with IC50 values of 1.5, 59, 580 and >6200 nm for MEK5, ERK5, TGFbR1 and other closely related kinases respectively. Available package size: 5,10,50,100mg A10212 PD (CI-1040) A10453 A10704 A10705 A10957 Honokiol PD PD98059 U0126-EtOH

23 37 MAPK MAPK 38 The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do A12824 SCH A10824 SB Inhibitor Name MEK MEK1 MEK1/2 MEK2 MEK5 Other A10895 Pexmetinib (ARRY-614) AZD8330 ERK phosphorylation A10970 AMG 548 BI IC50: 25 nm IC50: 4 nm Aurora B,Aurora C,Aurora A A10982 VX-702 Binimetinib IC50: 12 nm IC50: 7 nm BIX IC50: 4.3 nm ERK5,TGFβR1 BIX IC50: 1.5 nm ERK5,TGFβR1 Cobimetinib IC50: 4.2 nm GDC-0623 IC50: 0.13 nm Honokiol Akt-phosphorylation PD IC50: 0.33 nm PD IC50: 17 nm IC50: 17 nm PD PD98059 IC50: 2 μm Pimasertib IC50: 5 nm-2 μm Refametinib IC50: 19 nm IC50: 47 nm RO RO IC50: 5nM RO (CH ) IC50: 160 nm BRAF, CRAF Selumetinib IC50: 14 nm SL-327 IC50: 0.18 μm IC50: 0.22 μm AP-1,MKK3/p38 MAPK TAK-733 IC50: 3.2 nm Trametinib IC50: 0.92 nm IC50: 1.8 nm U0126-EtOH IC50: 0.07 μm IC50: 0.06 μm MKK6/p38 MAPK,MKK3/p38 MAPK A11029 GSK (JTP-74057, Trametinib) Sci Rep. 2016; 6: GSK purchased from Adooq ERK The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do SCH is a novel, specific inhibitor of ERK1/2 with IC50 of 4 nm and 1 nm, respectively. Available package size: 5,10,25,50mg A13420 GDC0994 A13977 TMCB A14090 XMD A14119 FR A15802 DEL A16231 APS-2-79 A16232 ERK5-IN-1 A16233 Tomatidine p38-mapk The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name p38 MAPK p38α p38β Other AL 8697 IC50: 6 nm AMG 548 Ki: 0.5 nm Ki: 3.6 nm Oncogene Jan 12; 31(2): VX-702 purchased from Adooq VX-702 is an orally bioavailable inhibitor of p38 MAP kinase that inhibits platelet agonist induced p38 activation (IC50= 4 to 20 nm). Available package size: 10,50,100,200mg A10983 VX-745 A11078 PH Nat Med Oct; 20(10): PH purchased from Adooq PH is a diarylpyridinone inhibitor of p38 mitogen-activated protein (MAP) kinase. Available package size: 5,10,50,100mg A11101 SKF Dihydrochloride A11221 PD GSK (JTP-74057) strongly prevented the activities of MEK1 and MEK2 kinases rather than activities of other 98 kinases. Available package size: 5,10,25,50mg A11040 TAK-733 A11247 RO A11264 Refametinib A11441 GDC-0973 (Cobimetinib) A11493 MEK162 (ARRY , Binimetinib) A12866 Refametinib (RDEA-119, BAY ) A12974 GDC-0623 A13119 Balamapimod (MKI-833) A13272 RO A13750 Hypothemycin A14019 RO (CH ) A14137 SL-327 A14380 G-479 A15050 Cobimetinib (racemate) A15051 Cobimetinib (R-enantiomer) A15157 MEK inhibitor A15762 BI A16032 PD A16044 PD Inhibitor Name ERK1 ERK2 ERK5 ERK Other DEL ERK5-IN-1 FR GDC-0994 Pluripotin (SC-1) SCH Ki: 0.31 μm Ki: 0.14 μm IC50: 1.1 nm Kd: 98 nm IC50: 4 nm Ulixertinib VX-11e IC50: 0.3 nm IC50: 1 nm IC50: <0.3 nm Ki: <2 nm XMD8-92 A11225 A11609 A11794 A12505 IC50: 0.5 μm IC50: 162 nm Kd: 80 nm Pluripotin (SC-1) XMD8-92 Ulixertinib (BVD-523, VRT752271) TCS ERK 11e (VX-11e) IC50: 0.5 μm RasGAP GSK3,AURA, CDK2 Sci Rep. 2017; 7: TCS ERK 11e purchased from Adooq TCS ERK 11e (VX-11e) is a potent and selective extracellular signalrelated kinase 2 (ERK2) inhibitor (Ki values are <2, 395, 540 and 852 nm for ERK2, GSK-3, Aurora Kinase A and Cdk2 respectively). Potently blocks proliferation of HT29 cells (IC50 = 48 nm). Available package size: 10,25,50,100mg BMS IC50: 13 nm Doramapimod Kd: 0.1 nm JX 401 IC50: 32 nm Losmapimod pki: 8.1 pki: 7.6 LY IC50: 7 nm ML-3043 IC50: 0.38 μm IL-1β, TNF-α Pamapimod IC50: 14 nm IC50: 480 nm PD IC50: 89 nm Pexmetinib Tie-2 PH IC50: 26 nm IC50: 102 nm RWJ IC50: 1 μm IC50: 11 μm SB IC50: 50 nm IC50: 100 nm SB IC50: μm PKB SB IC50: 44 nm IC50: 44 nm SB IC50: 19 nm IC50: 1 μm SD-06 IC50: 170 nm Skepinone-L IC50: 5 nm SX 011 IC50: 9 nm TAK-715 IC50: 7.1 nm IC50: 0.20 μm Talmapimod IC50: 9 nm VX-702 IC50: 4-20 nm VX-745 IC50: 10 nm IC50: 220 nm A10092 Asiatic acid A10148 Doramapimod (BIRB-796) A10545 LY A10823 SB PLoS One. 2016; 11(1): e SB purchased from Adooq Available package size: 10,50,100,200mg PLoS One. 2014; 9(12): e PD purchased from Adooq PD (PD169316) is a selective inhibitor of p38 MAPK.1 that inhibits p38 MAPK with an IC50 of 89 nm. Available package size: 5,10,25,50mg A11321 Skepinone-L A11562 SB A11563 SD-06 A11582 TAK-715 A12021 Asiaticoside A12408 ML-3043 A12526 Losmapimod (GW856553X) A12770 Talmapimod (SCIO-469) A13551 Pamapimod (R-1503) A13552 RWJ A13553 Dilmapimod A13563 BMS A13678 SB A16015 AL 8697 A16035 SX 011 A16037 EO 1428 A16038 JX 401 A16040 CMPD-1 A16055 SB A16058 DBM 1285 dihydrochloride A16236 TA-01

24 39 MAPK MAPK 40 JNK/c-Jun The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name JNK1 JNK2 JNK3 JNK Other IQ-1S IC50: 390 nm IC50: 360 nm IC50: 87 nm AS (Bentamapimod) IC50: 80 nm IC50: 90 nm IC50: 230 nm BI-78D3 IC50: 280 nm CC-401 CC-930 ( Tanzisertib) IC50: μm IC50: μm IC50: μm CEP-1347 IC50: 20 ± 2 nm DB07268 IC50: 9 nm IQ 3 Kd: 240 nm Kd: 290 nm Kd: 66 nm NF-κB, AP1 JNK Inhibitor IX pic50: 6.5 pic50: 6.7 JNK-IN-7 IC50: 1.5 nm IC50: 1.99 nm IC50: 0.75 nm IRAK1, PIK3C3, PIP5K3 and PIP4K2C JNK-IN-8 IC50: 4.7 nm IC50: 18.7 nm IC50: 1 nm Kit (V559D,T670I),Kit (V559D),RIOK2 SP IC50: 40 nm IC50: 40 nm IC50: 90 nm IC50: 0.4 μm Aurora A,TrkA,FLT3 SU 3327 IC50: 0.7 μm TCS JNK 6o IC50: 2 nm IC50: 4 nm IC50: 52 nm Vacquinol-1 A10860 SP is a JNK inhibitor with IC50=40 nm for JNK-1 and JNK-2 and 90 nm for JNK-3. Available package size: 10,25,50,200mg A11271 Anisomycin A11281 AEG 3482 A11296 AS (Bentamapimod) A11352 CC-401 A11969 TCS JNK 5a A12749 JNK-IN-8 A13564 CC-930 (Tanzisertib) A13565 CEP-1347 A13683 BI-78D3 A15037 CC-401 hydrochloride A15061 DB07268 A15136 JNK-IN-7 A15883 Vacquinol-1 A16020 SR 3576 A16036 IQ 3 A16039 SU 3327 A16041 JIP-1 ( ) A16045 c-jun peptide A16054 TCS JNK 6o A16059 DTP3 A16062 IQ-1S AP-1 A14950 SR A16305 SP PNRI-299 Int J Oncol Mar; 44(3): SP purchased from Adooq Raf A10001 A10002 Sorafenib (Nexavar) PLX-4720 Mol Cancer. 2011; 10: 114. PLX-4720 purchased from Adooq PLX-4720 is a B-raf inhibitor with IC50 of 160 nm. Available package size: 10,25,50,100mg A10250 Regorafenib (BAY ) A10420 GDC-0879 A10661 NVP-BHG712 A10739 PLX4032 (Vemurafenib) Sci Rep. 2016; 6: PLX4032 purchased from Adooq PLX4032 (Vemurafenib) also known as RG7204, Vemurafenib, R7204; RO PLX4032 is a B-raf inhibitor with an IC50 of 44 nm. Available package size: 10,50,100,200mg A10773 RAF265 (CHIR-265) A10774 Raf265 derivative A10829 SB A11063 AZ628 A11077 ZM A11211 ML 786 dihydrochloride A11240 MLN2480 (BIIB-024) A11333 BRAF inhibitor A11381 Dabrafenib (GSK A) A11436 GW 5074 A12739 PF A12891 Diazepinomicin A13119 Balamapimod (MKI-833) The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name Raf C-Raf/Raf-1 B-Raf A-raf Other AZ 628 IC50: 29 nm IC50: 34 nm CEP Kd: 39 nm Kd: 14 nm RET,PDGFRβ,LCK Dabrafenib IC50: 5.0 nm IC50: 0.8 nm Encorafenib EC50: 4 nm GDC-0879 IC50: 0.13 nm GW5074 IC50: 9 nm L IC50 = 10 nm p38α, GSK3β, Lck ML 786 dihydrochloride IC50: 2.5 nm MLN2480 B-Raf,IC50: 4.2nM; B-Raf(V600E), IC50: 2.1nM Abl-1, DDR2, EPHA2, RET, PERK NVP-BHG712 IC50: μm EphB4,c-Src,c-Abl PF IC50: 0.39 nm B-Raf,IC50: 0.19nM; BRAFV599E, IC50: 0.13nM PLX-4720 IC50: 6.7 nm IC50: 13 nm BRK,FRK,CSK PLX7904 RAF265 IC50: 3 nm-60 nm VEGFR2 Regorafenib (BAY ) IC50: 2.5 nm B-Raf,IC50: 28nM; B-Raf(V600E), IC50: 19nM FGFR1, Kit, PDGFRβ, RET, Tie-2, VEGFR1, VEGFR2, VEGFR3 RO IC50: 56 nm IC50: 8.2 nm MEK1 SB Ki: 0.16 nm Sorafenib IC50: 6 nm IC50: 38 nm mvegfr2(flk1),mvegfr3,mpdgfrβ TAK-632 IC50: 1.4 nm IC50: 8.3 nm Aurora B,PDGFRβ,FGFR3 Vemurafenib IC50: 48 nm IC50: 100 nm SRMS,ACK1,MAP4K5 (KHS1) ZM IC50: 70 nm A13135 Kobe0065 A13226 LGX 818 (Encorafenib) A13323 TAK-632 A13525 L A13772 CEP A14019 RO (CH ) A14122 B-Raf-inhibitor 1 A15040 CEP hydrochloride A15058 Dabigatran ethyl ester A15059 Dabrafenib Mesylate A15855 PLX7904 A16022 HG TOPK A14331 OTS964 A16023 OTS514 A16042 HI TOPK 032 JAK Detailed product information is on Page 4. Stat A10087 A10244 A10395 Artesunate Cryptotanshinone Fludarabine Phosphate (Fludara) MNK A13883 CGP A15362 Cercosporamide MLK A14219 URMC-099 Oncogenesis Jun; 6(6): e345. URMC-099 purchased from Adooq URMC-099 is an orally bioavailable, brain penetrant MLK inhibitor with IC50 of 19 nm, 42 nm, 14 nm, and 150 nm, for MLK1, MLK2, MLK3, and DLK, respectively. Available package size: 10,25,50,100mg KLF A15866 JAK / Stat ML264 A10396 Fludarabine (Fludara) A10817 S3I-201 (NSC 74859) S3I-201 (NSC 74859) is a novel inhibitor of Stat3 that inhibits Stat3, Stat3 complex formation and Stat3-DNA binding activity in vitro (IC50 = 86 ± 33 µm) and Stat3- dependent transcriptional activities. Available package size: 5,10,50,100mg

25 41 JAK / Stat Cell Cycle 42 The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name STAT1 STAT3 STAT5 Other Artesunate Corylifol A IC50: 0.8 um Cryptotanshinone IC50: 4.6 μm Cucurbitacin I JAK2 Fludarabine HO-3867 Napabucasin Nifuroxazide S3I-201 IC50: 86 μm SD 1008 JAK2 SH-4-54 Kd: 300 nm Kd: 464 nm Stattic IC50: 5.1 μm EXP1(a membrane glutathione S-transferase) ZM JAK3, EGFR, JAK1, CDK4 A12733 Chk The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name Chk1 Chk2 Other AZD7762 IC50: 5 nm BML-277 IC50: 15 nm CCT IC50: 3 nm CCT IC50: nm CHIR-124 IC50: 0.3 nm IC50: nm FLT3,PDGFR,GSK-3 LY IC50: 7 nm MK-8776 IC50: 3 nm IC50: 1.5 μm CDK2 PF Ki: 0.49 nm Ki: 47 nm VEGFR2,Fms,YES SB IC50: 15 nm cdc2, PKC A10113 Stattic AZD7762 Stattic is a small molecule shown to selectively inhibit the activation of the Stat3 transcription factor by blocking phosphorylation and dimerization events. Available package size: 50mg Oncol Lett Sep; 14(3): AZD7762 purchased from Adooq AZD7762 is a potent ATP-competitive checkpoint kinase inhibitor that drives checkpoint abrogation and potentiates DNA-targeted therapies. Available package size: 5,10,25,100mg A11036 LY (IC-83) LY is a chk2 inhibitor that binds to and inhibits the activity of chk2, which may prevent the repair of DNA caused by DNAdamaging agents. Available package size: 5,10,50,100mg A13474 A13628 A14249 Pim Cell Cycle Napabucasin STAT5 Inhibitor SH-4-54 A14264 HO-3867 A14490 Homoharringtonine A14701 Nitidine chloride A15363 Cucurbitacin I A15364 SD 1008 A15366 ZM A15729 Corylifol A A15885 STA-21 A16220 Nifuroxazide Detailed product information is on Page 5. A11046 CHIR-124 A11108 CCT A11167 SCH (MK-8776) A11520 PF A12703 SCH (S-isomer) A13575 BML-277 A13684 LY A14178 GNE-900 A15038 CCT hydrochloride A15480 SB A15550 CCT A15863 PD CDK A10093 AT7519 SH-4-54 is a potent STAT inhibitor with KD of 300 nm and 464 nm for STAT3 and STAT5. Available package size: 5,10,25mg CHIR-124 is a novel and potent Chk1 inhibitor (IC50: 0.32 nm and 697 nm for Chk1 and Chk2 respectively). Available package size: 5,10,25,100mg PLoS One. 2016; 11(2): e AT7519 purchased from Adooq AT7519 is an inhibitor of multiple cyclin-dependent kinases (CDKs), which may result in cell cycle arrest, induction of apoptosis, and inhibition of tumor cell proliferation. Available package size: 5,25,50,100mg The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name A abemaciclib AMG-925 AT7519 AT7519 HCl AZD5438 BMS BS-181 HCl CGP60474 CVT 313 Dinaciclib Flavopiridol Flavopiridol HCl Indirubin JNJ K03861 Kenpaullone CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CLK CDK Cdc Other IC50: 2.22 μm IC50: 210 nm IC50: 210 nm IC50: 16 nm IC50: 6 nm IC50: 20 nm IC50: 4.2 μm IC50: 3 nm IC50: 40 nm IC50: 40 nm IC50: 9 nm IC50: 0.4μM Ki: 46 nm IC50: 47 nm IC50: 47 nm IC50: 6 nm IC50: 9 nm IC50: 50 nm IC50: 0.5 μm IC50: 1 nm IC50: 40 nm IC50: 40 nm IC50: 4 nm Kd: 15.4 nm IC50: 0.68μM LDC IC50: μm IC50: μm LY (abemaciclib) LY Milciclib MK-8776 ML167 NU 6102 NU2058 NU6027 P Palbociclib HCl Palbociclib Isethionate PHA PHA Purvalanol A R547 Ribociclib Ro-3306 Roscovitine SNS-032 SU9516 TG003 THZ1 Wogonin XL413 A10163 A10390 A10471 A10494 A10701 A10716 IC50: 398 nm IC50: 9.5 nm IC50: 26 μm Ki: 2.5 μm IC50: 79 nm IC50: 250 nm IC50: 60 nm Ki: 2 nm Ki: 20 nm IC50: 480 nm IC50: 40 nm IC50: 363 nm IC50: 0.16 μm IC50: 5.4 nm IC50: 17 μm Ki: 1.3 μm IC50: 224 nm IC50: 240 nm IC50: 8 nm IC50: 70 nm Ki: 3 nm IC50: 0.7 μm IC50: 38 nm IC50: 22 nm IC50: 2 nm IC50: 3 nm IC50: 100 nm IC50: 360 nm IC50: 100 nm IC50: 58 nm IC50: 230 nm IC50: 215 μm IC50: 40 nm IC50: 360 nm IC50: 40 nm BS-181 HCl Flavopiridol (Alvocidib) Indirubin JNJ PD HCl (Palbociclib) PHA IC50: 253 nm IC50: 13 nm IC50: 13 nm IC50: 1 nm IC50: 0.85μM IC50: μm IC50: 2 nm IC50: 160 nm IC50: 1.6 μm IC50: 63 nm IC50: 11 nm IC50: 9 nm IC50: 62 nm IC50: 850 nm Ki: 1 nm IC50: 925 nm IC50: 200 nm IC50: 265 nm IC50: 10 nm IC50: 170 nm IC50: 2.4 μm IC50: 170 nm IC50: 2.4 μm IC50: 40 nm IC50: 40 nm IC50: 175 nm IC50: 10 nm IC50: 21 nm IC50: 300 nm IC50: 300 nm IC50: 246nM IC50: 150 nm IC50: 396 nm IC50: 2.87 μm IC50: 15 nm IC50: 15 nm IC50: 460 nm IC50: 5 nm IC50: 0.16 μm IC50: 340 nm IC50: 10 nm IC50: 62 nm IC50: 3.2 nm IC50: <10 nm IC50: <10 nm IC50: 20 nm IC50: 4 nm IC50: 44 nm IC50: 16nM IC50:11nM IC50: 20 nm IC50: 34 nm IC50: 138 nm IC50: 4 nm IC50: 1522 nm IC50: 15 nm A10806 Roscovitine (Seliciclib) A10850 SNS-032 (BMS ) A11034 A A11045 Flavopiridol HCl A11047 PHA (Milciclib) A11105 AZD5438 IC50: 5 μm IC50: 10 nm IC50: 10 nm IC50: 4 nm Akt1,PKA,GSK-3β FLT3 GSK-3β GSK-3β PKCα GSK-3β Aurora A,Aurora B,VEGFR2 GSK-3β,ERK2,c- Src TrkA Chk1,Chk2 DNA topoisomerase II ATPase ATR,DNA-PK GSK-3β,PKCα,c- Src GSK-3β, MK2, PLK1 GSK-3β GSK-3β PKCδ, SGK, ERK ERK2, GST-ERK1, IC50: 0.65 μm ERK1 IC50: 3.4 nm IC50: 3.4 nm GSK-3α,GSK-3β PDGFR Pim1,CK2

26 43 Cell Cycle Cell Cycle 44 A11129 Dinaciclib (SCH ) A14427 Palbociclib A10452 HMN-214 A15178 Narciclasine A11154 BMS A10673 ON A15225 ROCK inhibitor A11164 A11167 PHA SCH (MK-8776) Cell Cycle, 2014, 13(23), Palbociclibe purchased from Adooq A15226 A15239 ROCK inhibitor-1 SLx-2119 (KD025) A11190 R547 A15888 Ripasudil A11220 Kenpaullone A15921 SAR HCl A11313 A11347 A11962 A12216 A12352 AT7519 HCl CGP60474 TG-02 (SB1317) Wogonin Purvalanol B A12438 NU 6102 A12494 A12584 A12742 A12989 A13130 A13506 NG52 ON BAY (Roniciclib) LY (abemaciclib) RGB AZD5597 A13524 NSC A13547 P A13549 A13550 A13677 A13721 A13811 LEE011 (Ribociclib) PHA BMS (XL-413) TG003 PD Isethionate Molecular cancer therapeutics, 2014, 13(4), PD Isethionate purchased from Adooq PD Isethionate is a highly selective inhibitor of CDK4/6 with IC50 of 11 nm/16 nm respectively. Available package size: 10,25,50mg A14025 A14136 A14192 AMG-925 NU6027 THZ1 Palbociclib is an orally available pyridopyrimidine-derived cyclindependent kinase (CDK) inhibitor with potential antineoplastic activity. Available package size: 10,25,50mg A14437 Ro 3306 A15005 AT7519 trifluoroacetate A15039 CDK9 inhibitor 2 A15054 CVT-313 A15196 NVP-LCQ195 A15485 AG A15517 Purvalanol A A15767 NU2058 A15823 LY A15889 K03861 A15942 Bohemine A16325 LY A16386 LY methanesulfonate Aurora Kinase Detailed product information is on Page 5. PLK The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name PLK1 PLK2 PLK3 Other BI 2536 IC50: 0.83 nm IC50: 3.5 nm IC50: 9.0 nm GSK Ki: 2.2 nm GW843682X IC50: 2.2 nm IC50: 9.1 nm HMN-214 MLN0905 IC50: 2 nm NMS-P937 IC50: 2 nm Rigosertib IC50: 9 nm PI3Kα, Met, Tie-2 ON is selectively cytotoxic for chronic lymphocytic leukemia cells through a dual mechanism of action involving PI3K/AKT inhibition and induction of oxidative stress. Available package size: 5,10,50,100mg A11146 TAK-960 A11438 GW843682X A12429 MLN 0905 A13045 NMS A13245 RO3280 A14426 SBE 13 HCl A16261 LFM-A13 ROCK The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name ROCK ROCK1 ROCK2 Other AT13148 IC50: 6 nm IC50: 4 nm PKA,p70S6K,Akt1 Fasudil HCl Ki: 330 nm PKA,PKG,PKC GSK IC50: 1.6 nm IC50: 4 nm MSK1,RSK1 GSK429286A IC50: 14 nm IC50: 63 nm KD025 IC50: 60 nm Ripasudil IC50: 51 nm IC50: 19 nm RKI-1447 IC50: 14.5 nm IC50: 6.2 nm Thiazovivin IC50: 0.5 μm Y HCl Ki: 140 nm Ki: 300 nm A10381 A10441 Fasudil HCl (HA-1077) GSK429286A GSK429286A is a cell-permeable, selective small molecule inhibitor of Rho-associated, coiled-coil containing protein kinase (ROCK). Available package size: 5,25,50,100mg A16211 c-myc LX7101 A F4 A16324 KJ Pyr 9 Wee1 A10599 A15863 Ras MK-1775 PD A10107 Azathioprine A11010 Zoledronic Acid A11572 Salirasib A12546 NSC A12578 Kobe2602 A12740 EHop-016 A13112 GGTI-2418 A13119 Balamapimod (MKI-833) A13135 Kobe F4 is a c-myc inhibitor that prevents c-myc/max dimerization. Available package size: 25, 50,100mg MK-1775 is a potent and selective Wee1 kinase inhibitor in vitro and in vivo. Available package size: 5,10,25, 50mg Cell Rep Oct 10; 21(2): THZ1 Isethionate purchased from Adooq Ro3280 IC50: 3 nm SBE 13 HCl IC50: 200 pm IC50: 875 nm TAK-960 IC50: 0.8 nm IC50: 16.9 nm IC50: 50.2 nm Volasertib IC50: 0.87 nm A10134 BI 2536 A10928 Thiazovivin A11001 Y HCl A11610 Y A12348 GSK A12464 AT13148 Kobe0065 inhibits anchorage-dependent and -independent growth, blocks MEK/ERK activity and induces apoptosis in H-rasG12V transformed NIH3T3 cells. Available package size: 10,25,50mg THZ1 is a novel selective and potent covalent CDK7 inhibitor with IC50(binding affinity) of 3.2 nm; inhibits Jurkat cell's proliferation with IC50 of 50 nm. Available package size: 5,10,25mg A14273 LDC A14297 ML167 A14318 SU9516 A14392 Voruciclib A14414 CA-224 BI 2536 is a selective inhibitor of Plk1, which inhibits Plk1 enzyme activity at low nanomolar concentrations. Available package size: 5,10,50,100mg A10135 A10442 BI6727 (Volasertib) GSK A12674 SR 3677 dihydrochloride A13067 RKI-1447 A13659 Glycyl-H HCl A13785 HA-1077 dihydrochloride A15045 chroman 1 A15101 H-1152 A15102 H-1152 dihydrochloride A15118 Hydroxyfasudil A15119 Hydroxyfasudil hydrochloride A13403 ZCL-278 A13886 EHT 1864 A13975 NSC HCl A14103 K-Ras(G12C) inhibitor 6 A14227 K-Ras(G12C) inhibitor 12 A H05 (trifluoroacetate salt) A14250 K-Ras(G12C) inhibitor 9 A14430 CCG-1423 A14956 BQU57

27 45 Cell Cycle DNA Damage 46 A15925 ML-098 A12922 ID 8 A12856 Gimatecan A10221 Cisplatin A16049 XRP44X A14314 AZ191 A13059 Beta-Lapachone A16097 A16175 A H05 APS-2-79 HCl AMI5 A16255 Mirk-IN-1 G-quadruplex A13443 A13656 A13780 BNS-22 CKD602 Ellipticine Oncotarget Jan 26; 7(4): Cisplatin purchased from Adooq DYRK A12438 NU 6102 HDAC Detailed product information is on Page 1. PARP Detailed product information is on Page 3. DNA-PK Detailed product information is on Page 19. Topoisomerase The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name Topoisomerase Topo I Topo II Topo IV Other Adriamycin Amonafide Amrubicin Beta-Lapachone IDO1 Betulinic acid Camptothecin Daunorubicin HCl Doxorubicin Epirubicin HCl Etoposide Flumequine Gatifloxacin Ki: 20 nm IC50: 5 μm IC50: 0.68 μm IC50: 15 μm A12717 A14975 A14976 Pyridostatin 360A 360A iodide DNA Damage HIV-1, Aminopeptidase N Genistein EGFR Idarubicin HCl IC50: 3.3 ng/ml Multicellular spheroids Irinotecan Irinotecan HCl Trihydrate Marbofloxacin Mitoxantrone Mitoxantrone HCl Moxifloxacin HCl Ofloxacin Pirarubicin Podophyllotoxin SN-38 Teniposide Topotecan HCl IC50: 13 nm A10005 (-)-Epigallocatechin gallate A10023 ABT-492 (Delafloxacin) A10041 Adriamycin A10071 Amonafide (AS1413) A10174 Camptothecin A10194 Cerubidine A10345 Epirubicin HCl A10373 Etoposide (VP-16) A10419 Gatifloxacin A10426 Genistin (Genistoside) A10465 Idarubicin HCl A10478 Irinotecan A10479 Irinotecan HCl Trihydrate A10557 Marbofloxacin A10595 Mitoxantrone A10596 Mitoxantrone Hydrochloride A10609 Moxifloxacin HCl A10652 Norfloxacin (Norxacin) A10666 Ofloxacin (DL8280) A10735 Pirarubicin A10740 Podophyllotoxin A10907 Teniposide A10939 Topotecan HCl (Hycamtin) A11231 Exatecan mesylate A11658 Balofloxacin A11659 Sarafloxacin HCl A11861 Flumequine A11902 Pefloxacin mesylate A11997 (S)-10-Hydroxycamptothecin A11999 Betulinic acid A12011 SN 38 PLoS One. 2018; 13(1): e SN 38 purchased from Adooq SN 38 is the active metabolite of irinotecan (an analog of camptothecin - a topoisomerase I inhibitor). Available package size: 50,100,250mg A12569 A12663 Ametantrone Amrubicin A13993 A14141 A14158 A14363 A14403 A15064 A15280 A15467 A15837 A16167 A16458 Telomerase A10140 BIBR 1532 ATM / ATR NK314 TAS 103 2HCl Voreloxin Nemorubicin Doxorubicin ABT 492 meglumine Voreloxin Hydrochloride Clorobiocin SW Levofloxacin hydrate Clinafloxacin DNA, RNA Synthesis A10036 A10042 A10152 A10182 A10214 Cycloheximide (Actidione) Fluorouracil (Adrucil) Bleomycin sulfate Carboplatin Cidofovir (Vistide) Ellipticine is a DNA intercalating agent and a DNA topoisomerase II inhibitor. Available package size: 25,50,100mg Neurosci Lett Aug 26;629: BIBR 1532 purchased from Adooq BIBR 1532 is a selective telomerase inhibitor (IC50 values are 93, > and > nm for human telomerase, human RNA polymerase I and human RNA polymerase II + III respectively). Available package size: 10,50,100,200mg A10240 Costunolide A13093 Amsacrine A13206 GENZ A Thio-dG A16354 RHPS4 Detailed product information is on Page 20. J Phys Chem B Sep 3; 119(35): Cidofovir (Vistide) purchased from Adooq Cidofovir (Vistide) is an antiviral used for the treatment of cytomegalovirus (CMV) infection (ie: retinitis). Available package size: 50,100,200mg Cisplatin was the first member of a class of platinum-containing anti-cancer drugs, which now also includes carboplatin and oxaliplatin. These platinum complexes react in vivo, binding to and causing crosslinking of DNA, which ultimately triggers apoptosis (programmed cell death). Available package size: 250,2000mg A10224 A10228 A10281 A10289 A10346 A10392 A10395 A10407 A10423 A10466 A10532 A10535 A10568 A10597 A10632 A10948 A11065 Clafen (Cyclophosphamide) Clofarabine Dacarbazine Daptomycin Oxaliplatin (Eloxatin) Floxuridine Fludarabine Phosphate (Fludara) Tegafur Gemcitabine HCl (Gemzar) Ifosfamide Lincomycin hydrochloride (U-10149A) Lomustine (CeeNU) Mercaptopurine Mizoribine Nelarabine (Arranon) Trifluridine CX-5461 Biology of Reproduction, Volume 94, Issue 4,1-12 CX-5461 purchased from Adooq CX-5461 is a first-in-class non-genotoxic small molecule targeted inhibitor of RNA polymerase I (Pol I) that activates the p53 pathway without causing DNA damage. Available package size: 5,10,50,100mg A11147 CCT A11179 NSC (XI-006) A11491 Mitomycin C A11612 YK A11803 Azithromycin (Zithromax) A11804 Adenine sulfate A12326 INNO-206 (Aldoxorubicin) A12406 Apaziquone A12409 Epirubicin Oncology reports, 2016, 35(1), Epirubicin purchased from Adooq Epirubicin is a cell-permeable antitumor antibiotic. A stereoisomer of Doxorubicin that exhibits reduced cardiotoxicity. Epirubicin s antitumor actions are mediated by targeting and inhibiting Topo II (topoisomerase II). Available package size: 10,25,50,100mg

28 47 DNA Damage DNA Damage 48 A12773 A12890 A13285 A14199 A14212 A14230 A14252 A14268 A14301 A14304 A14306 A14378 A14440 A15447 A15533 A15790 A15898 A15978 A16114 A16194 A16203 A16208 Bleomycin hydrochloride Thiostrepton Tubercidin 4EGI-1 Blasticidin S HCl Mupirocin Chloroambucil Puromycin 2HCl 4E1RCat CRT Triapine Bleomycin E3330 SCR7 TAS-102 L189 6-Mercaptopurine Monohydrate L67 Saccharin 1-methylimidazole RK-33 AN2718 Chebulinic acid RNA/DNA Polymerase A10395 A10790 A10791 A10908 A11115 A11120 A11590 Fludarabine Phosphate (Fludara) Rifabutin Rifampin Tenofovir (Viread) Abacavir DNA alkylator A10059 A10124 A10930 A11635 Abacavir sulfate T-705 (Favipiravir) Altretamine Bendamustine HCl (SDX-105) Thiotepa PloS one, 2014, 9(7), e T-705 (Favipiravir) purchased from Adooq T-705, a substituted pyrazine compound, has been found to exhibit potent anti-influenza virus activity in vitro and in vivo. Available package size: 10,25,50,100mg A11596 Triptolide (PG490) A13239 Actinomycin D A13274 Delavirdine mesylate A14335 BMH-21 A15270 Valaciclovir A15333 Oncrasin 1 A15385 Mithramycin A A15386 Thiolutin Cyclophosphamide monohydrate A13473 A15162 A15269 A15344 Synthases / Synthetases A10050 A10776 A11113 A11488 Alendronate sodium hydrate Raltitrexed (Tomudex) Pneumocandin B0 MF63 A12258 HPGDS inhibitor 1 A12992 A13261 A13269 A13270 MTH1 A14291 A15536 A15537 Sirtuins HQL-79 Nolatrexed Dihydrochloride Caspofungin Micafungin (S)-crizotinib TH287 TH588 Detailed product information is on Page6. IRE1 A13803 A13828 Uramustine Miriplatin hydrate VAL-083 Melphalan 4μ8C APY29 Genetics, 2016, 202(4), Micafungin purchased from Adooq A13436 Anidulafungin A13483 YM A13999 Triacsin C A14107 C75 A14937 Bismuth Subcitrate Potassium A14938 Bismuth Subsalicylate A15331 C 75 A15442 Genz free base A15466 Eliglustat tartrate A16202 Buthionine Sulphoximine A16329 AN3365 Available package size: 1,2,5,10mg Nat Chem Biol Dec; 8(12): APY29 purchased from Adooq APY29 inhibits IRE1α autophosphorylation (IC50 = 280 nm) and activates IRE1α RNase activity. Available package size: 10,25,50mg DNA Stain A15072 Dye 937 A15103 HOE A15104 HOE A15105 HOE A15106 Hoechst A15107 Hoechst analog A15108 Hoechst analog 2 A15109 Hoechst analog 3 Microtubules A10014 A Demethylepipodophyllotoxin ABT-751 (E-7010) ABT-751 is an antimitotic agent, inhibits microtubule polymerization, binds to β-tubulin on the colchine site; blocks cell cycle at G2M phase and induces apoptosis. Available package size: 10,50,100,200mg A10049 A10204 A10238 A10264 A10326 A10359 A10360 A10689 A10740 A10973 A10975 A10976 A11412 A11449 A11617 A11831 A12591 A12601 A12804 Albendazole Chloroxine Colchicine CYT997 (Lexibulin) Docetaxel (Taxotere) Epothilone A Epothilone B (EPO906) Paclitaxel (Taxol) Podophyllotoxin Vincristine sulfate Vinflunine Tartrate Vinorelbine (Navelbine) Epothilone D Ixabepilone Vincristine Cabazitaxel Cevipabulin (TTI-237) Combretastatin A4 Eribulin Mesylate A15110 Hoechst analog 5 A15111 Hoechst analog 6 A15112 Hoechst A15113 Hoechst analog A15114 Hoechst analog 2 A15115 Hoechst A15116 HOE-S A15158 meta-iodohoechst A15193 Nuclear yellow A15199 ortho-iodohoechst A15206 para-iodohoechst Cytoskeleton PLoS One. 2017; 12(8): e ABT-751 (E-7010) purchased from Adooq CYT997 is a novel anti-cancer vascular disrupting agent (VDA). In vitro, CYT997 is shown to potently inhibit the proliferation of vascular endothelial growth factor-stimulated human umbilical vein endothelial cells (IC(50) 3.7 ± 1.8 nm) and cause significant morphological changes at 100 nm, including membrane blebbing. Available package size: 5,10,50,100mg A12954 PAK A11930 A12553 A13691 A13838 Monomethyl auristatin E Monomethyl auristatin E (MMAE) is an antimitotic agent which inhibits cell division by blocking the polymerisation of tubulin, and also shows inhibition of antibody-drug conjugates (ADCs) activity. Available package size: 5,10,25,50mg A13081 Fosbretabulin disodium (CA4P) A13219 Nocodazole A13268 Ansamitocin P-3 A13661 Vinblastine sulfate A13735 CW069 A13827 CK-636 A13872 INH1 A14200 INH6 A14295 Vinorelbine Tartrate A14328 Sagopilone A14362 VcMMAE A14442 D A14665 Cucurbitacin B A Epi 10-Desacetyl Paclitaxel A xylosyltaxol A15070 Docetaxel Trihydrate A15156 Mc-MMAD A15172 MMAD A15273 Vc-MMAD A15455 ELR A15960 DM1-Sme A16124 TRx0237 (LMTX) mesylate PF FRAX597 FRAX486 LOR-253 Journal of Immunotherapy, 2016, 39(6), Monomethyl auristatin E purchased from Adooq

29 49 Cytoskeleton Cell Metabolism 50 Dynamin The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name Dynasore IC50: ~15 μm Mdivi-1 IC50: 1-10 μm Dyngo-4a IC50: 0.38 μm A12726 Integrin A11614 Dynasore Zaurategrast (CDP323) Oncogene Mar; 36(11): FRAX597 purchased from Adooq FRAX597, a small-molecule pyridopyrimidinone, is a potent and ATP competitive inhibitor of the group I PAKs (PAK1 IC50= 8 nm, PAK2 IC50= 13 nm, PAK3 IC50= 19 nm). Available package size: 5,10,25mg A15506 KPT-9274 Dynamin JBC. 2016, 291(47), Dynasore purchased from Adooq Dynasore is a non-competitive inhibitor of dynamin 1, dynamin 2 and mitochondrial dynamin (Drp1) GTPase activity. Available package size: 10,25,50,100mg A14316 A14867 A15915 Mdivi-1 Dynamin inhibitory peptide Dyngo-4a Front Immunol Oct 20;6:525. Zaurategrast (CDP323) purchased from Adooq CDP323 is a small-molecule prodrug antagonist of the vascular cell adhesion molecule 1 binding to alpha4-integrins. Available package size: 5,10,25,50mg A12371 A12372 Cilengitide trifluoroacetate Cilengitide OncoTargets and therapy, 2016, 9: Cilengitide purchased from Adooq Cilengitide is a cyclic Arg-Gly-Asp peptide with potential antineoplastic activity. Cilengitide binds to and inhibits the activities of the alpha(v)beta(3) and alpha(v)beta(5) integrins, thereby inhibiting endothelial cell-cell interactions, endothelial cell-matrix interactions, and angiogenesis. Available package size: 5,10,25,50mg A12787 Firategrast (SB ) A12876 Pyrintegrin A13968 Leukadherin 1 A14923 Cyclo (-RGDfK) A15456 E7820 A15538 A15918 A15967 Kinesin The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name ARQ 621 RGD (Arg-Gly-Asp) Peptides Cyclo(RGDyK) CWHM12 AZ 3146 IC50: ~35 nm GSK Ki: 3.2 nm Ispinesib Ki app: 1.7 nm MPI IC50: 1.8 nm SB IC50: 14.4 nm A10486 Ispinesib (SB ) A10828 SB Mps1 A11170 AZ 3146 A11218 Mps1-IN-1 A14290 MPI Gap Junction Protein A11593 Tonabersat (SB ) A14865 Gap 26 A14866 Gap 27 Kinesin Oncotarget Nov 3; 8(54): SB purchased from Adooq SB , a second generation KSP inhibitor, is a highly potent and active therapeutic in preclinical models of cancer. Available package size: 5,10,50,100mg A11050 Arry-520 (Filanesib) A11170 AZ 3146 A11435 GSK A11976 Monastrol A13735 CW069 A14234 ARQ 621 A14290 MPI A15001 ARRY-520 R enantiomer A15841 Dimethylenastron A15844 K 858 A15956 EMD A14876 A14920 A14921 A15091 A15092 Sci Rep. 2017; 7: Gap 27 purchased from Adooq Available package size: 5,10,25mg GnRH Associated Peptide (GAP) (1-13), human 10Panx Scrambled 10Panx GAP-134 (Danegaptide) GAP-134 Hydrochloride Cytochrome P450 A10020 A10054 A10081 A10102 A10120 A10200 A10225 A10234 A10293 A10489 A10498 A10578 A10625 A10688 A10744 A10853 A10978 A11044 A11058 A11138 A11144 Abiraterone (CB-7598) Alizarin Apigenin Avasimibe (CI-1011) Baicalein Chloramphenicol Clarithromycin Clotrimazole Deferasirox Itraconazole (Sporanox) Ketoconazole Methoxsalen (Oxsoralen) Naringenin Ozagrel(OKY-046) Posaconazole Sodium Danshensu Voriconazole (Vfend) TAK-700 (Orteronel) Abiraterone Acetate (CB7630) TOK-001 (Galeterone) TH-302 (Evofosfamide) Cell Metabolism Oncotarget Dec 29; 8(70): TH-302 purchased from Adooq TH-302 is a selectively targeting hypoxic regions of solid tumors hypoxia-activated prodrug. Available package size: 5,10,50,100mg A11277 Cobicistat (GS-9350) A11409 Cyproterone acetate A11481 Luliconazole A11865 Hydroxyflutamide (Hydroxyniphtholide) A11977 TMS A12544 PF A13113 Talarozole A13361 ABT A Cyano-7-ethoxycoumarin A13366 Mephenytoin A13367 Methoxyresorufin A13515 TAK-700 Salt (Orteronel Salt) A15010 Azathramycin A15044 Choline Fenofibrate A15826 Efavirenz PLoS Pathog Dec; 13(12): e Efavirenz purchased from Adooq Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI). Available package size: 10,25,50mg A16201 A16449 PPAR Benzbromarone Chlorzoxazone A10385 Fenofibrate A10424 Gemfibrozil (Lopid) A10807 Rosiglitazone (BRL-49653) A10809 Rosiglitazone maleate A11137 Cetaben A11437 GW A11588 T A11680 Pioglitazone (Actos) A11727 Ciprofibrate A11981 Troglitazone A11982 GW 7647 A11983 L-165,041 A11984 GW 9662 A12360 pirinixic acid (WY 14643) A12391 GSK-3787 GSK-3787 is a potent and selective peroxisome proliferator-activated receptor δ (PPARδ) antagonist (pic50 = 6.6). Available package size: 5,25,50,100mg A12392 GSK 0660 Mol Endocrinol Sep; 27(9): GSK 0660 purchased from Adooq GSK 0660 is a selective PPARβ antagonist (IC50 values are 0.155, > 10 and 10 µm at PPARβ, PPARα and PPARγ respectively). Available package size: 10,25,50,100mg A12413 GW6471 A12492 Aleglitazar A14958 GW0742 elife. 2017; 6: e GW0742 purchased from Adooq GW0742 is a selective agonist of PPARδ with EC50 value of 1.1 nm. Available package size: 10,25,50mg A15013 A15044 A15099 A15129 A15454 Balaglitazone Choline Fenofibrate GW1929 Inolitazone dihydrochloride Elafibranor

30 51 Cell Metabolism Cell Metabolism 52 A15836 A16001 A16307 PDE The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name PDE PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE9A PDE10A Other Aminophylline AN2728 Apremilast Avanafil Bay Cilomilast Cilostamide Cilostazol Deltarasin Dipyridamole Dyphylline GSK Ibudilast (KC-404) Icariin Irsogladine Luteolin Milrinone MK-0359 Nortadalafil Oglemilast Olprinone HCl PF PF PF-8380 Pimobendan Roflumilast Rolipram Sildenafil Tadalafil TAK-063 Vardenafil IC50: 0.12 mm Kd: 38 nm Autotaxin, IC50: 2.8 nm Ki: 15.0 μm IC50: 180 nm IC50: 20 nm Ki: 6.4 μm IC50: 0.11 µm IC50: 74 nm IC50: 100 nm PDE3A, IC50: 27 nm; PDE3B, IC50: 50 nm; IC50: 0.2 μm Ki: 13.9 μm IC50: 5.2 μm IC50: 2.1 μm IC50: 0.32 μm IC50: 3.2 pm Ki: 11.1 μm IC50: 1 nm IC50: μm Ki: 9.5 μm PDE4B, IC50: 2.5 nm; PDE4D IC50: 1.7 nm IC50: 0.7 nm IC50: 2.0 μm IC50: 3.5 nm IC50: 1.8 nm IC50: 0.7 nm IC50: 33 nm IC50: 12 nm IC50: 0.37 nm IC50: 0.3 nm adenosine receptor machr,achr Vinpocetine Sodium channel Zardaverine A10066 A10216 A10217 A10319 A10339 A10449 A10464 BMS Fenofibric acid Bezafibrate Aminophylline Cilomilast (SB ) Cilostazol Dipyridamole Dyphylline Hesperetin Icariin IC50: 0.5 μm IC50: 0.8 μm Icariin is inhibitory to all three PDE5 isoforms that inhibits PDE5A1, A2, and A3. Available package size: 5,10,25,50mg A16308 A16309 A16463 A10480 A10541 A10592 A10733 A10804 CDDO-Im DG172 dihydrochloride Clofibric Acid Irsogladine Luteolin Milrinone (Primacor) Pimobendan (Vetmedin) Roflumilast ATPase Roflumilast acts as a selective, long-acting inhibitor of the enzyme PDE-4. Available package size: 5,10,50,100mg A10805 A10883 A10965 A11019 A11073 A11191 Rolipram Tadalafil Vardenafil Ibudilast (KC-404) GSK PF Oncotarget Feb 2; 7(5): PF purchased from Adooq PF is a phosphodiesterase inhibitor selective for the PDE10A subtype. Available package size: 5,10,50,100mg A11289 Apremilast (CC 10004) A11326 Bay A11527 PF-8380 HSP A11602 A12550 A12619 A12631 A12776 A13121 A13467 A13596 A13722 A15097 A15191 A15197 A15198 A15546 A15799 A16142 Vinpocetine Zardaverine Avanafil Sildenafil AN2728 PF MK-0359 Cilostamide Deltarasin HCl GSK ,2,2-trifluoroacetic acid Nortadalafil Oglemilast Olprinone Hydrochloride HA130 TAK-063 Sildenafil Mesylate The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name HSP70 HSP90 HSP90α HSP90β HSP105 Other Alvespimycin HCl IC50: 62 nm BIIB021 EC50: 38 nm CH Kd: 0.48 nm Kd: 0.48 nm CUDC-305 (DEBIO-0932 ) EC 144 Ki: 0.2 nm and IC50: 1.1 nm Ganetespib IC50: 4 nm Geldanamycin Kd: 1.2 μm p185 HSP990 IC50: 0.8 nm IC50: 0.6 nm IC50: 0.8 nm IPI-493 Ki: 21 nm IPI-504 (Retaspimycin HCl) KNK437 KW-2478 IC50: 3.8 nm Luminespib IC50: 13 nm IC50: 13 nm IC50: 21 nm Macbecin I IC50: 2 μm MKT 077 MPC-3100 IC50: 60 nm NMS-E973 DC50: <10 nm NVP-BEP800 IC50: 58 nm IC50: 58 nm Onalespib IC50: 18 nm PF Kd: 41 nm HER2 PU-H71 IC50: 51 nm SNX-2112 Ka: 30 nm Ka: 30 nm Ka: 30 nm Tanespimycin IC50: 5 nm TRC VER IC50: 0.5 μm VER IC50: 47 nm IC50: 47 nm VER IC50: 21 nm IC50: 21 nm XL888 IC50: 24 nm A AAG (KOS953) A DMAG HCl (Alvespimycin) A10143 BIIB021 Sci Rep. 2017; 7: AAG (KOS953) purchased from Adooq 17-AAG is an ansamycin antibiotic which acts as an anti-tumor agent. Specifically, 17-AAG binds and inhibits Hsp90. Available package size: 5,10,50,100mg Nat Commun. 2017; 8: 451. BIIB021 purchased from Adooq BIIB021 is an oral fully synthetic Hsp90 inhibitor that selectively and potently inhibits the molecular chaperone Hsp90 thereby inhibiting the proper assembly of multiple oncogenic proteins involved in tumor growth and survival. Available package size: 5,10,50,100mg

31 53 Cell Metabolism Cell Metabolism 54 A10343 A10659 A10660 A11025 A11062 A11074 A11130 A11131 A11189 A11195 A11251 A11269 A11272 A11402 A11768 Hydroxylases A10485 A10542 A10637 A10920 A11172 Elesclomol (STA-4783) AUY922 (NVP-AUY922) NVP-BEP800 Geldanamycin AT13387 PF (SNX-5422) PU-H71 MPC-3100 SNX-2112 KW-2478 XL-888 IPI-504 (Retaspimycin HCl) IPI-493 Ganetespib (STA-9090) Radicicol A12388 MKT 077 A12648 CUDC-305 (DEBIO-0932 ) A12765 A12850 Rocaglamide HSP-990 A13351 VER A13667 A13812 A13817 A14129 A14282 A14292 A14389 A14990 A16034 A16050 Geranylgeranylacetone VER VER PU-WS13 CH NMS-E973 KNK437 Alvespimycin Gedunin Macbecin I A16053 TRC A16056 EC 144 A16347 AUY922 (NVP-AUY922) is highly potent and oral inhibitor of Hsp90 with IC50=21 nm in Hsp90 FP binding assay and inhibits proliferation of various human cancer cell lines in vitro, with GI50 average 9 nm. Available package size: 5,10,25,100mg KRIBB11 Isotretinoin LX 1606 Hippurate Nepicastat (free base) (SYN-117) Tetrahydropapaverine HCl Nepicastat HCl Journal of Virology, 2017, pii: e VER purchased from Adooq VER is a small molecule, ATP-derivative inhibitor of HSP70 (IC50 = 500 nm). Available package size: 10,25,50,100mg A11371 Collagen proline hydroxylase inhibitor A11785 LX 1606 A12833 Ro A13363 Metyrapone A13998 DMOG DMOG is a cell permeable, competitive inhibitor of HIF-PH. It acts to stabilize HIF-1α expression at normal oxygen tensions in cultured cells, at concentrations between 0.1 and 1 mm. Available package size: 100,200mg A14013 LCI-699 (Osilodrostat) A14299 Telotristat Etiprate A14325 LP A14602 Panaxtriol A Chloro-DL-phenylalanine Factor Xa The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name Factor Xa Other Apixaban Ki: 0.08 nm Edoxaban Ki: nm Thrombin,FIXa Rivaroxaban IC50: 0.7 nm Prothrombinase A10082 MAO Apixaban (BMS ) A10158 BMS A10800 Rivaroxaban (Xarelto) A11517 Otamixaban (FXV 673) A12411 Rivaroxaban Diol A12518 Betrixaban A12870 Razaxaban A12871 Letaxaban (TAK-442) A13878 ABT333 A14099 DPC-423 A14317 Edoxaban A R-Rivaroxaban A15076 Edoxaban tosylate The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name MAO-A MAO-B MAO Other Moclobemide IC50: 6.1 μm Paeonol IC50: 54.6 μm IC50: 42.5 μm Rasagiline Mesylate IC50: 412 nm IC50: 4.43 nm Safinamide Mesylate IC50: 580 μm IC50: 98 nm Nat Commun. 2018; 9: 295. DMOG purchased from Adooq Apixaban is an anticoagulant for the prevention of venous thromboembolism and venous thromboembolic events. Available package size: 5,10,50,100mg Tranylcypromine HCl CYP2A6 A10454 A10765 A10766 DHFR Hordenine Quercetin dihydrate (Sophoretin) Quercetin (Sophoretin) Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C. Available package size: 100,500mg A10818 Safinamide Mesylate (FCE28073) A11111 Rasagiline A11722 Rasagiline mesylate A11777 SL A11885 Moclobemide A13294 Safinamide A13353 Bifemelane HCl A13358 Tranylcypromine hydrochloride A C-C HCl A C-I HCl A14344 RN-1 2HCl A15761 Olodaterol The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Methotrexate Inhibitor Name DHFR Other Pemetrexed Ki: 7.2 nm TS,GARFT Pemetrexed Disodium Hydrate Ki: 7.2 nm TS,GARFT Pralatrexate A10021 A10655 A10707 A11522 A11787 A12668 A12796 A15207 Dehydrogenases A10070 A10192 A10320 Methotrexate (Abitrexate) NSC (DAMPA) Pemetrexed (Alimta) Pemetrexed is chemically similar to folic acid and is in the class of chemotherapy drugs called folate antimetabolites. It works by inhibiting three enzymes used in purine and pyrimidine synthesis thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase. Available package size: 10,50,100,200mg Pralatrexate Aminopterin Pemetrexed disodium Trimetrexate Pemetrexed disodium hemipenta hydrate Ammonium Glycyrrhizinate (AMGZ) Celastrol Disulfiram The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name Dehydrogenase AGI-5198 IC50: 0.16 μm AGI-6780 IC50: 23 nm Ammonium Glycyrrhizinate CPI-613 Disulfiram Emodin Enoxolone Gimeracil Gossypol Acetate Leflunomide MK-8245 IC50: 1 nm Mycophenolate Mofetil IC50: 39 nm NCT-501 IC50: 40 nm PluriSIn #1 (NSC 14613) SW Ki: 0.1 nm Trilostane Vidofludimus IC50: 134 nm A10353 A10435 A10521 A10613 A10780 A10949 A11403 A11682 A11786 A12385 A12442 Glycyrrhetinic acid (Enoxolone) Gossypol Leflunomide Mycophenolate mofetil (CellCept) Ranolazine Trilostane MK-8245 Gimeracil CPI-613 CGP 3466B maleate Brequinar J Cancer. 2017; 8(15): Brequinar purchased from Adooq Brequinar is an inhibitor of dihydroorotate dehydrogenase, an enzyme that is required for de novo pyrimidine biosynthesis. Available package size: 5,10,25,50mg A12902 AGI-5198 (IDH-C35) AGI-5198, also know as IDH-C35, is the a very potent and selective mutant IDH1 inhibitor that was shown to potential anticancer activity. Available package size: 5,10,25,50mg A12903 AGI-6780 A12925 JK 184 A12997 Vidofludimus (4SC-101) A13542 AZD4017 A14386 AG-120 AG-120 is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity. Available package size: 5,10,25mg

32 55 Cell Metabolism Cell Metabolism 56 A14412 A14599 ASP9521 Monoammoniumglycyrrhizinate A12166 A12652 Mogroside II A2 T HMG-CoA Reductase A10894 A10944 Tazarotene Tretinoin A15170 MK-8245 Trifluoroacetate A12865 Cerpegin A11094 Bexarotene (LGD1069) A15798 SW A15805 Alda 1 A15808 Enasidenib A15869 AG-120 A15892 NCT-501 A15100 A15241 A15535 FAAH GW3965 Sobetirome SR9243 The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name HMG-CoA Reductase Atorvastatin Calcium Clinofibrate IC50: 0.47 mm Lovastatin IC50: 3.4 nm A11298 Adarotene (ST1926) A11589 Tamibarotene A11792 AM 580 A11793 CD 437 A12163 Fenretinide A16164 Fomepizole A16176 CBR 5884 A11049 URB597 Mevastatin Pravastatin sodium IC50: 5.6 μm Rosuvastatin Calcium IC50: 11 nm Procollagen C-proteinase A10959 UK Carbonic Anhydrase Sci Rep. 2017; 7: URB597 purchased from Adooq URB597 is a relatively selective inhibitor of the enzyme fatty acid amide hydrolase (FAAH). Available package size: 5,25,50,100mg A11183 PF-3845 A10737 A10810 A11800 A11877 A11912 A12128 Pitavastatin calcium (Livalo) Rosuvastatin calcium (Crestor) Atorvastatin calcium Lovastatin (Mevacor) Pravastatin sodium Swertiamarin Fenretinide is a synthetic retinoid agonist. It is an antiproliferative, antioxidant and anticancer agent with a long half-life in vivo. Available package size: 25,50,100mg A12430 Palovarotene A12905 AR7 The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name Carbonic Anhydrase Brinzolamide Acetazolamide IC50: 10 nm Benzenesulfonamide Dichlorphenamide Dorzolamide HCl Tioxolone U-104 Carbonic Anhydrase I Ki: 6000 nm Ki: 91 nm Carbonic Anhydrase II IC50: 3.19 nm Carbonic Anhydrase IV Ki: 36 nm Ki: 1.9 nm Ki: 31 nm Ki: 5.08 μm Ki: 9.64 μm A10303 Diclofenamide A10333 Dorzolamide HCL A11673 Tioxolone A11765 Brinzolamide A12105 Punicalagin A12106 Punicalin A12325 Indisulam (E7070) A13594 Benzenesulfonamide A14410 DTP348 A14959 U-104 A15859 Acetazolamide Carbonic Anhydrase IX Carbonic Anhydrase XII Ki: 45.1 nm Ki: 4.5 nm A11960 LY A12390 JZL195 A12420 JNJ A15209 PF A15954 JNJ CETP The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name CETP Anacetrapib (MK-0859) rhcetp, IC50: 7.9 nm; Mutant CETP (C13S), IC50: 11.8 nm Evacetrapib (LY ) IC50: 5.5 nm JTT-705 (Dalcetrapib) rhcetp, IC50: 0.2 μm Torcetrapib (CP ) IC50: 37 nm A11084 Anacetrapib (MK-0859) PLoS One. 2017; 12(8): e Anacetrapib (MK-0859) purchased from Adooq Anacetrapib (MK-0859) is a CETP inhibitor being developed to treat hypercholesterolemia (elevated cholesterol levels) and prevent cardiovascular disease. Available package size: 5,10,50,100mg A11213 JTT-705 (Dalcetrapib) A13709 A13743 A13896 FXR A11141 Mevastatin Atorvastatin Pitavastatin Lactone GW4064 A11186 WAY A12547 Lithocholic acid A13866 Obeticholic Acid A16077 DY 268 IDO A13004 BMC Biol. 2017; 15: 120. GW4064 purchased from Adooq GW4064 is a selective, non-steroidal farnesoid X receptor (FXR) agonist (EC50 = 15 nm). Available package size: 10,50,100,200mg INCB analog A13007 TTNPB PLoS One. 2017; 12(11): e TTNPB purchased from Adooq TTNPB enhances reprogramming efficiency in chemically induced pluripotent stem cells (CiPSCs). Available package size: 10,25,50mg A14127 LG A16292 AGN A16293 AGN A16294 AGN A16295 AGN A16296 AGN A16356 Etretinate Lipase A10229 Clofibrate A10676 Orlistat A10890 Tanshinone IIA (Tanshinone B) A11095 URB754 A12390 JZL195 A12747 JZL184 LXR A11204 GW3965 HCl A11242 A11397 Ferroptosis Torcetrapib (CP ) Evacetrapib (LY ) A14322 NLG919 A14397 Indoximod (NLG-8189) A15121 IDO inhibitor 1 A15554 Epacadostat (INCB024360) JZL184 is a potent and selective MAGL inhibitor. Blocks hydrolysis of the endocannabinoid 2-arachidonyl glycerol (2-AG) in vivo in the mouse brain (IC50 = 8 nm). Cell Feb 27;156(5): GW3965 HCl purchased from Adooq GW3965 HCl is a selective and orally active liver X receptor (LXR) full agonist. Available package size: 5,10,50,100mg A13247 A13822 A15865 Ferrostatin-1 (Fer-1) Erastin RSL3 RSL3 is a ferroptosis activator in a VDAC-independent manner,exhibiting selectivity for tumor cells bearing oncogenic RAS. Available package size: 5,10,25mg Retinoid Receptor A10035 A10038 Acitretin Adapalene Epacadostat is a potent and selective indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 of 10 nm, Phase 2. Available package size: 5,10,25mg A13150 A13774 A13814 A14704 A15944 A16081 A16359 XEN445 JW-642 Atglistatin Dihydroberberine Cetilistat (ATL-962) MJN110 URB602 Available package size:10,25,50,100mg

33 57 Cell Metabolism Cell Metabolism 58 Phospholipases A12581 P7C3-A20 LDL A12368 FTI 277 A14020 LB42708 A10206 A10548 Chlorpromazine hydrochloride LY (Varespladib) Jpn J Ophthalmol Mar;61(2): P7C3-A20 purchased from Adooq A10379 A11084 Ezetimibe (Zetia) Anacetrapib (MK-0859) A14439 A15796 FTI-277 HCl L HCl Infection and immunity, 2016, 84(2), LY purchased from Adooq LY (Varespladib) is an inhibitor of the IIa, V, and X isoforms of secretory phospholipase A2 (spla2). Available package size: 5,10,50,100mg A10741 Polydatin (Piceid) A10765 Quercetin dihydrate (Sophoretin) A10766 Quercetin (Sophoretin) A10889 Tanshinone I A11388 D609 A13411 Isotetrandrine A13895 FIPI A14274 Darapladib A14339 U A15390 TCS 401 A16338 ML348 A16462 Clofazimine Lipoxygenase A11725 Edaravone (MCI-186) A12061 Ginkgetin A12879 Tepoxalin A13346 MK 886 A14400 AZD6642 A ,7-Dihydroxycoumarin A14994 AM679 A15163 MK-0591 (Quiflapon) A15169 MK591 A15190 Nordihydroguaiaretic acid A15818 GSK AhR A12945 StemRegenin 1 (SR1) P7C3-A20 is a potent neuroprotective agent. Available package size: 5,10mg A12934 P7C3 A12937 (R)-P7C3-Ome A13318 GNE-617 A14072 STF GLUT A15552 STF-31 STF-31 is an inhibitor of glucose transporter 1 (GLUT1, IC50 = 1 mum). Available package size: 10,25,50mg A15877 WZB117 Antimetabolite A10177 A10183 A10223 A10251 A10286 A10292 A10395 A10396 A15980 A15981 Lipid Metabolism A12318 Capecitabine (Xeloda) Carmofur Cladribine Flupirtine maleate Daphnetin Decitabine Fludarabine Phosphate (Fludara) Fludarabine (Fludara) Lometrexol disodium LY SC Neuronal Metabolism A11751 A15815 Foxo1 A15871 DGAT Probucol ETC-1002 A11199 A Farnesyl Transferase A10935 AS AS is a cell-permeable inhibitor that blocks the transcription activity of Foxo1 with IC50 of 33 nm. It could directly bind to the active Foxo1, but not the Ser256-phosphorylated form. Available package size: 5,25,50mg A is a diacylglycerol acyltransferase 1 (DGAT-1) inhibitor (IC50 values are 7 and 24 nm at human and mouse DGAT-1). Available package size: 5,10,50,100mg A11526 PF A14984 ABT-046 A15012 AZD7687 A15067 DGAT-1 inhibitor 2 A15919 Xanthohumol ETC-1002 is a novel, first-in-class, orally available, once-daily LDL-C lowering small molecule; activator of hepatic AMP-activated protein kinase (AMPK); also has potent inhibitory activity against hepatic ATP-citrate lyase(ic50=29 um). Available package size: 5,10,25mg Tipifarnib (Zarnestra) Journal of pharmaceutical sciences, 2015, 105(2), A purchased from Adooq Sci Rep. 2017; 7: Tipifarnib (Zarnestra) purchased from Adooq CRM1 A14124 Piperlongumine A16078 KPT 335 A16341 KPT276 Thioredoxin A13831 PX 12 A16122 CCF642 Vitamin A10458 Hydroxocobalamin (Vitamin B12a) A11346 Calcipotriol A11367 Calcifediol A11533 Paricalcitol A12227 Folic acid A12489 MC-976 A13788 Vatiquinone A14960 (24R)-MC 976 A14961 (24S)-24,25-Dihydroxyvitamin D3 A14962 (24S)-MC 976 A alpha, 24, 25-Trihydroxy VD2 A alpha, 25-Dihydroxy VD2-D6 A alpha-Hydroxy VD4 A , 25-Dihydroxy VD2 A , 25-Dihydroxy VD3 A Hydroxy VD2-D6 A O-(2-Aminoethyl)-25-hydroxyvitamin D3 A15032 Calcifediol monohydrate A15123 Impurity B of Calcitriol A15124 Impurity C of Alfacalcidol A15125 Impurity C of Calcitriol A15126 Impurity of Calcipotriol A15153 Maxacalcitol A15237 Secalciferol J Stem Cells Regen Med. 2017; 13(2): StemRegenin 1 (SR1) purchased from Adooq StemRegenin 1 (SR1) is a cell-permeable purine derivative that acts as an antagonist of aryl hydrocarbon receptor and promotes the selfrenewal of hematopoietic stem cells (HSCs). Available package size: 10,25,50,100mg A15436 CH A12404 ONO 2506 SREBP A11230 PF Nature cell biology, 2013, 15(12), PF purchased from Adooq Tipifarnib (Zarnestra) is a farnesyltransferase inhibitor that inhibits the Ras kinase in a post translational modification step before the kinase pathway becomes hyperactive. Available package size: 5,10,25100mg A12328 Lonafarnib (SCH66336) A15251 A15252 A15274 A15278 A15905 A16199 A16410 Tacalcitol Tacalcitol monohydrate VD2-D3 Vitamin D4 Calcium D-Panthotenate Pyridoxamine 2HCl Amprolium HCl A15913 NAMPT A12515 UM171 CHS-828 (GMX1778) PF is a reversible, competitive inhibitor of sterol regulatory element-binding protein (SREBP) site 1 protease. Available package size: 10,25,50,100mg A16121 Fatostatin Lonafarnib (SCH 66336) is a selectively FPTase inhibitor for H-ras, K-ras-4B and N-ras with IC50 of 1.9 nm, 5.2 nm and 2.8 nm, respectively. Available package size: 5,10,25100mg Decarboxylase A10125 Benserazide HCl (Serazide) A10181 Carbidopa A16174 Eflornithine hydrochloride hydrate

34 59 Autophagy Signaling Autophagy Signaling 60 Autophagy A10785 A10866 A11656 A12234 A12942 LRRK2 A10662 Resveratrol STF Autophagy Signaling Flubendazole (Flutelmium) Scutellarein Spautin-1 Spautin-1 is a novel autophagy inhibitor, IM inhibited the growth of K562 cells with IC50 of 1.03μM. In contrast, co-treatment with Spautin-1 increased IM-induced inhibition of cell viability with IC50 of 0.45 μm. Available package size: 10,25,50mg A14208 A14287 Hydroxychloroquine Sulfate PFK15 PFK15 is a potent and selective 6-phosphofructo-2-kinase (PFKFB3) with IC50 of 207 nm. Available package size: 25,50,100mg A15769 A15795 SBC SBI SBI is a potent, selective and cell permeable autophagy kinase ULK1 inhibitor with IC50 of 108 nm for ULK1 kinase activity and 711 nm for the highly related kinase ULK2 Available package size: 5,10,25mg A15867 SMER28 A15880 A16358 A16421 A16445 TAE684 PLoS Genet Aug; 13(8): e SBI purchased from Adooq SMER28 is a small-molecule enhancer (SMER) of autophagy, inducing autophagy independently of rapamycin in mammalian cells. Available package size: 10,25,50mg MRT68921 Lys05 Azithromycin Dihydrate Chloroquine Phosphate TAE684 is a inhibitor of ALK and also a potent inhibitor of LRRK2 kinase activity (IC(50) of 7.8nM against wild-type LRRK2, 6.1nM against the G2019S mutant). Available package size: 5,10,50,100mg A11477 A12798 A12919 CXCR LRRK2-IN-1 GSK A HG A13448 CZC A13748 GNE-7915 A13969 GNE0877 A14149 GNE 9605 A15504 PF A15510 A15777 CZC54252 hydrochloride JH-II-127 The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name CXCR1 CXCR2 CXCR4 Other AMD 070 IC50: 13 nm AMD-070 HCl IC50: 13 nm ATI-2341 EC50: 194 nm MSX-122 IC50 : 10 nm Plerixafor IC50: 44 nm CXCL12- mediated chemotaxis Plerixafor 8HCl IC50: 44 nm CXCL12- mediated chemotaxis Reparixin IC50: 1 nm IC50: 100 nm CXCL8 SB IC50: 22 nm SB IC50: 22 nm SCH IC50: 1.3 nm IC50: 7.3 nm SCH IC50: 42 nm IC50: 3 nm WZ811 EC50: 0.3 nm A10913 Plerixafor 8HCl (DB06809) A11097 SRT3109 A11315 AMD 070 HG is a brain penetrant, potent and selective inhibitor of wildtype LRRK2. Available package size: 2,5,10mg PF is a highly potent, selective, brain penetrant LRRK2 inhibitor with IC50 of 3 nm/11 nm for Wt LRRK2/G2019S LRRK2 respectively. Available package size: 10,25,50mg BMC cancer, 2016, 16(1), 305. AMD 070 purchased from Adooq AMD 070 is a CXCR4 chemokine receptor antagonist. Available package size: 5,10,25,50mg A11555 A11577 A11953 A12383 A12588 A12596 A13074 IL Receptor A10881 A11462 A11963 A13478 A13794 A15426 A15999 A16268 A16414 COX A10030 A10090 A10193 SCH (Navarixin) SRT3190 AMD 3465 Hexahydrobromide Reparixin WZ811 MSX-122 AMD3100 (Plerixafor) BMC cancer, 2016, 16(1), 305. AMD3100 (Plerixafor)purchased from Adooq Plerixafor is an immunostimulant used to multiply hematopoietic stem cells and it is a chemokine receptor-4 antagonist for mobilization of hematopoietic stem cells for transplantation. Available package size: 10,25,50,100mg A14195 SB Immunology & Inflammation Suplatast tosilate IRAK-1-4 Inhibitor I Y320 MCC950 sodium Apilimod beta-interleukin I ( ), human YM APY0201 AS101 Acetaminophen Asaraldehyde (Asaronaldehyde) Celecoxib Celecoxib is a sulfa non-steroidal anti-inflammatory drug (NSAID) and selective COX-2 inhibitor. Available package size: 100,500,1000mg A10304 Diclofenac sodium A10461 Ibuprofen (Advil) A10462 Ibuprofen Lysine (NeoProfen) A10474 Indomethacin (Indocid, Indocin) A10623 Naproxen sodium A10720 Phenylbutazone (Butazolidin, Butatron) A10736 Piroxicam (Feldene) A10749 Pravadoline (WIN 48098) A10878 Sulindac (Clinoril) A11464 Iguratimod (T 614) A11641 Pranoprofen A11686 Flunixin meglumine A14209 The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name COX COX-1 COX-2 Other Acemetacin Amfenac Sodium Monohydrate Asaraldehyde Aspirin Bromfenac Sodium IC50: 250 nm IC50: 150 nm Carprofen IC50: 30 nm Celecoxib IC50: 40 nm Diclofenac Sodium IC50: 60 nm IC50: 200 nm Ibuprofen IC50: 13 μm IC50: 370 μm Ibuprofen Lysine Indomethacin IC50: 0.28 μm IC50: 14 μm Lornoxicam IC50: 5 nm IC50: 8 nm Meclofenamate Sodium IC50: 40 nm IC50: 50 nm Meloxicam Naproxen Sodium IC50: 8.7 μm IC50: 5.2 μm Nepafenac Nimesulide IC50: 26 μm Phenacetin Piroxicam Pranoprofen Rofecoxib IC50: 18 nm Sulindac SB SB is a potent, and selective CXCR2 antagonist with IC50 of 22 nm for inhibiting interleukin IL-8 binding to CXCR2, > 150-fold selectivity over the other 7-TMRs tested. Available package size: 10,25,50mg A14997 AMD-070 HCl A15219 Reparixin L-lysine salt A15234 SCH A15439 UNBS5162 A15941 AZD-5069 A16351 ATI-2341 Tolfenamic Acid IC50: 0.2 μm Valdecoxib IC50: 5 nm A11692 A11693 A11694 A11695 A11697 Acemetacin (Emflex) Tolfenamic acid Nimesulide Lornoxicam (Xefo) Licofelone Anat Cell Biol Dec; 50(4): Licofelone purchased from Adooq Licofelone is a dual COX/LOX inhibitor, being considered as a treatment for osteoarthritis. Available package size: 5,10,50,100mg

35 Immunology & Inflammation Immunology & Inflammation A11768 A11859 A11906 A11918 A11986 A12043 A12434 A12520 A12879 Radicicol Fexofenadine HCl Phenacetin Rofecoxib (Vioxx) ATB-337 (-)-Epicatechin (S)-(+)-Flurbiprofen Meclofenamate Sodium Tepoxalin A13023 SC 560 A13116 A13244 NS-398 A13332 FK 3311 A13342 A13572 Bromfenac sodium Valdecoxib Parecoxib Sci Rep. 2015; 5: Parecoxib purchased from Adooq Parecoxib is a potent and selective COX-2 inhibitor. Available package size: 10,25,50,100mg A13770 Etoricoxib A13983 ATB 346 A15205 Paradol A15919 Xanthohumol A16002 Fenbufen A16166 Diflunisal A16399 Amfenac Sodium Monohydrate A16409 Ampiroxicam A16428 Carprofen CCR A10556 Maraviroc (UK ) Maraviroc is an antiretroviral drug in the CCR5 receptor antagonist class used in the treatment of HIV infection. Available package size: 5,25,50,100mg A10971 Vicriviroc Malate Antimicrobial agents and chemotherapy, 2015, 59(12), Vicriviroc Malate purchased from Adooq Vicriviroc Malate is a second generation orally active CCR5 antagonist, which is also a potent inhibitor of HIV-1 entry into target cells, with a mean IC50 =0.46 nm and IC50 =1~10 nm to HIV isolates (n=52). Available package size: 5,10,50,100mg A11104 INCB 3284 dimesylate A11127 MK-0812 A11136 INCB8761 (PF ) A13471 Aplaviroc A13643 Cenicriviroc A13846 TAK-779 A14409 BX471 A15227 RS A15276 Vicriviroc maleate A15924 NSC5844 A16363 ZK dihydrochloride Toll-like Receptors A10469 A12548 A12683 A12841 A13251 CXCR Imiquimod (Aldara) Detailed product information is on Page 59. ROS A10032 A10055 A10056 A10252 A10382 A13053 NOS A12710 A13359 A13583 A13901 Keap1-Nrf2 A13164 A14417 Acetylcysteine Allopurinol Allopurinol sodium Dihydromyricetin (Ampeloptin) Febuxostat (TEI-6720) 6-Benzylaminopurine Gw Diphenyleneiodonium chloride 1400W Dihydrochloride Biopterin Oltipraz RTA-408 Imiquimod (Aldara) is a a heterocyclic imidazoquinoline amide that acts as an immune response modifier. Available package size: 100,250mg VGX-1027 Toll-Like Receptor 7 Ligand II VTX-2337 GS-9620 GS-9620 is a potent and selective orally active small molecule agonist of Toll-like receptor 7. Available package size: 5,10,25,50mg A14208 Hydroxychloroquine Sulfate A14351 Isatoribine A15253 TAK-242 S enantiomer A15264 Toll-like receptor modulator A15890 Resiquimod A16299 LTR CDDO-EA CDDO-EA is an activator of Nrf2/ARE; Neuroprotective effect. Available package size: 5,10,50mg A16300 NK-252 A11607 MK-0679 (Verlukast) A11908 Pranlukast (ONO 1078) A12529 MK-571 PLoS One. 2014; 9(12): e CDDO-EA purchased from Adooq Sci Rep. 2017; 7: MK-571 purchased from Adooq MK-571 is a potent CysLT1 (LTD4) leukotriene receptor inverse agonist with EC50 value of 1.3 nm. Available package size: 10,25,50mg A13090 LY A15983 MK-571 sodium salt MALT A12928 MI 2 PD-1/PD-L1 A15882 PD1-PDL1 inhibitor 1 A15906 PD1-PDL1 inhibitor 2 5-HT Receptors A hydroxytryptophan (5-HTP) A10048 Agomelatine A10091 Asenapine maleate A10222 Citalopram Hydrobromide A10231 Clomipramine HCl A10287 Dapoxetine hydrochloride A10437 Granisetron Hydrochloride A10497 Ketanserin (Vulketan Gel) A10588 Mianserin hydrochloride A10607 Mosapride citrate A10619 Naftopidil 2HCl A10624 Naratriptan A10667 Olanzapine (LY170053) A10674 Ondansetron HCl (GR 38032F) A10759 Puerarin (Kakonein) A10797 Risperidone (Risperdal) A10931 Tianeptine sodium NADPH oxidase A11989 Apocynin (Acetovanillone) A13359 Diphenyleneiodonium chloride A13360 ML 171 A14433 GKT GKT is a first in class inhibitor targeting NOX1 and NOX4 enzymes. Available package size: 5,10,25mg Immunology & Inflammation related A13333 Flufenamic acid A Deacetoxy Deflazacort A14285 CORM-3 A14562 Benzydamine HCl A14874 Anti-Inflammatory Peptide 1 A15312 SC 57461A A15434 Cyclosporine A15585 Aceneuramic acid hydrate A15754 Eugenol A16119 Escin A16139 Loxoprofen A16333 Prostaglandin F2 alpha GPCR / G Protein A11106 A11116 A11165 A11178 A11182 LY Vilazodone RS BRL WAY WAY was originally believed to act as a selective 5-HT1A receptor antagonist, but subsequent research showed that it also acts as potent full agonist at the D4 receptor. Available package size: 10,25,50mg A11208 BMY 7378 BMY 7378 is a 5-HT1A partial agonist and high affinity α1d adrenoceptor antagonist. Available package size: 10,50,200mg A11226 Tropisetron (ICS )

36 63 GPCR / G Protein GPCR / G Protein 64 A11310 Alosetron A15148 LY A11843 Carvedilol A16186 TAK 259 A11418 Eletriptan hydrobromide A15216 Quetiapine A11846 Dexmedetomidine HCl A16387 Acebutolol HCl A11538 Pardoprunox HCl (SLV-308) A15282 WAY maleate salt A11868 Ivabradine HCl (Procoralan) A16465 Clorprenaline HCl A11598 A11701 Tianeptine Ondansetron (Zofran) A15286 A15438 Ziprasidone SB HCl A11905 A11914 Procaterol HCl Prazosin HCl Histamine Receptors A11702 Mirtazapine A11703 Trazodone HCl A11704 Urapidil hydrochloride A11705 Duloxetine A11717 Duloxetine HCl A11743 Tegaserod maleate A11771 Prucalopride A11799 Almotriptan malate (Axert) A11801 Aripiprazole (Abilify) A11824 Blonanserin A11873 Lamotrigine A11925 SB HCl A12378 Lorcaserin A12397 Sibutramine hydrochloride A12521 Lu AE58054 (Idalopirdine) A12598 lorcaserin hydrochloride (APD-356) A12602 A13075 A13092 A13267 A13293 A13417 A13424 A13458 A13501 A13664 Vortioxetine (Lu AA21004) hydrobromide Eletriptan NAD 299 hydrochloride (Robalzotan) PRX Tandospirone NAN-190 hydrobromide Atomoxetine HCl Norfluoxetine S HCl Ketanserin tartrate A13757 PU 02 A13762 N-Desmethylclozapine A13766 SDZ HCl A13767 Tropanserin A13833 RU hemisuccinate A13860 Flibanserin A13865 Edivoxetine HCl A14026 SB HCl A14091 Bifeprunox Mesylate A14092 SB A14102 SB HCl A14163 WAY A14198 Lasmiditan A14255 Cyclobenzaprine HCl A14356 LuAE58054 A14375 Tropisetron HCL A14391 Levomilnacipran HCl A14434 Pimavanserin (ACP-103) A14989 Alosetron Hydrochloride A15002 Asenapine HCl A15048 Clozapine N-oxide A15096 Granisetron A15491 Desvenlafaxine succinate hydrate A15499 Ricasetron A15500 LY A15501 Lerisetron A15542 Piboserod A15592 BRL A15687 Buspirone HCl A15838 GSK A15884 Pimavanserin A15923 Eptapirone A16169 Cyproheptadine hydrochloride A16337 YL-0919 A16404 Amitriptyline HCl A16417 Azasetron HCl Adrenergic Receptors A10052 Alfuzosin HCl A10091 Asenapine maleate A10149 Bisoprolol fumarate A10232 Clonidine hydrochloride A10296 Dehydroepiandrosterone A10298 Detomidine hydrochloride A10325 Dobutamine hydrochloride A10334 Doxazosin mesylate A10484 Isoprenaline HCl A10555 Maprotiline hydrochloride A10618 Naftopidil (Flivas) A10619 Naftopidil 2HCl A10630 Nebivolol HCl A10686 Oxymetazoline hydrochloride A10719 Phenoxybenzamine hydrochloride A10794 Rilmenidine A10819 Salbutamol sulfate (Albuterol) A10843 Silodosin (Rapaflo) A10882 Synephrine (Oxedrine) A11229 Metroprolol succinate A11538 Pardoprunox HCl (SLV-308) A11666 Phenylephrine HCl A11668 DL-Adrenaline A11713 Metoprolol tartrate A11721 Betaxolol A11732 Formoterol hemifumarate A11733 Betaxolol hydrochloride A11734 Phentolamine mesilate A11740 Terazosin hydrochloride A11788 Salmeterol A11807 Adrenalone HCl A11923 Apalutamide (ARN-509) A11971 Diprophylline A12657 Tamsulosin A12795 Arformoterol tartrate A12844 Formoterol A12861 Mirabegron A13080 Tetrahydrozoline Hydrochloride A13225 ICI 118,551 hydrochloride A13399 BRL maleate A13401 Cimaterol A13406 Bisoprolol A13408 HEAT hydrochloride (BE 2254) A13409 Idazoxan Hydrochloride A13412 JP HCl A13417 NAN-190 hydrobromide A13419 Octopamine hydrochloride A13421 Phentolamine HCl A13422 Pindolol A13426 Rauwolscine A13427 S-(-)-Atenolol A13428 S(-)-Propranolol HCl A13429 (S)-Timolol maleate A13430 SR 59230A HCl A13432 Tulobuterol A13433 UK 14,304 tartrate A13434 Xylazine HCl A13623 Celiprolol HCl A13635 Guanabenz acetate A13657 CL disodium salt A13676 BRL Na Salt A13738 Nebivolol A13775 Medetomidine HCl A13902 Atipamezole HCl A14223 Salmeterol Xinafoate A14239 Labetalol HCl A14251 Bambuterol HCl A14258 Carteolol HCl A14936 Tamsulosin hydrochloride A14964 (R,R)-Formoterol A15002 Asenapine HCl A15033 Brimonidine Tartrate A15098 Guanfacine hydrochloride A15117 HOKU-81 A15266 Trenbolone A15491 Desvenlafaxine succinate hydrate A15878 ICI A15998 Vilanterol trifenatate A16170 Modafinil A10091 A10117 A10195 A10205 A10218 A10226 A10538 A10671 A11117 A11222 A11340 A11360 A11699 A11709 A11712 A11714 A11724 A11859 A11921 A12356 A12661 A12713 A12845 A13073 A13086 A13442 A13641 A13899 A14248 A14946 A15015 A15016 A15041 A15047 A15075 A15213 A15214 A15285 A15666 A16129 A16132 A16169 A16393 A16411 A16418 A16472 Asenapine maleate Azelastine HCl (Allergodil) Cetirizine Dihydrochloride Chlorpheniramine maleate Cimetidine Clemastine fumarate Loratadine Olopatadine hydrochloride Ciproxifan maleate Rupatadine Bepotastine Besilate Ciproxifan Brompheniramine Cyproheptadine hydrochloride Orphenadrine citrate Lafutidine Mizolastine Fexofenadine HCl Roxatidine acetate hydrochloride Rupatadine Fumarate Bilastine JNJ Bepotastine Clemizole Metiamide A HCl Immethridine hydrobromide Astemizole Promethazine HCl Ebastine Bavisant dihydrochloride Bavisant dihydrochloride hydrate Cetirizine Clemizole hydrochloride Ebrotidine Pitolisant hydrochloride Pitolisant oxalate Zaltidine Buclizine HCl CarbinoxaMine Maleate Lidocaine hydrochloride Cyproheptadine hydrochloride Alcaftadine Antazoline HCl Azatadine dimaleate Cyclizine 2HCl

37 65 GPCR / G Protein GPCR / G Protein 66 Opioid Receptors A10561 A11072 A11076 MCOPPB 3HCl ADL5859 HCl JTC-801 Mol Cell Biochem Jan;411(1-2): JTC-801 purchased from Adooq JTC-801 is a selective antagonist for the nociceptin receptor, also known as the ORL-1 receptor. Available package size: 5,10,50,100mg A11210 BRL HCl A11292 Alvimopan (ADL ) A11322 BAN ORL 24 A11718 Trimebutine A12579 Nalfurafine hydrochloride A13485 Kainic acid monohydrate A13758 SIB 1757 A13759 SIB 1893 A13854 A A14006 Ibotenic Acid A14330 JNJ A15053 CPPHA A15174 MTEP hydrochloride A15189 Noopept A15378 DL-AP3 A15811 CBiPES HCl A15832 VU A16108 (S)-3,5-DHPG Melatonin Receptors A10564 A10777 Melatonin Ramelteon (TAK-375) A12912 Platelet-Activating Factor (PAF) Receptors A10429 A11222 A11739 A12356 A14257 Ginkgolide B Rupatadine Ginkgolide A Rupatadine Fumarate Etizolam Endothelin Receptors A11006 CASIN CASIN is a novel and potent Cdc42 inhibitor. Available package size: 2,5,10mg A16432 CCG Zibotentan (ZD4054) Int J Mol Sci Mar; 18(3): 586. CASIN purchased from Adooq A13498 Cloprostenol (sodium salt) A13751 BAY-u 3405 A13880 NS-304 (Selexipag) A14600 Saikosaponin B2 A15525 GW A15532 MF498 A15853 CP (Taprenepag) A15964 Grapiprant (CJ ) A15968 TG Adenosine Receptors A10040 A10066 A10339 A11451 Adenosine Aminophylline Dyphylline Istradefylline (KW-6002) Nalfurafine hydrochloride is a kappaopioid receptor agonist. Available package size: 2,5,10,25mg Peptide Receptors A11820 Prostaglandin E1 (PGE1) A11979 YIL 781 A11091 Bosentan A11291 Ambrisentan (BSF ) World J Hepatol Aug 8; 8(22): Ambrisentan (BSF ) purchased from Adooq Istradefylline (KW-6002) is a selective antagonist at the A2A receptor. It has been found to be useful in the treatment of Parkinson's disease. Available package size: 5,10,25,50mg A13479 ADL5747 A13843 Nalmefene hydrochloride A14085 Eluxadoline A14187 U A14337 TRV130 (Oliceridine) A14991 Alvimopan dihydrate A14992 Alvimopan monohydrate A15149 LY A15159 Methylnaltrexone Bromide A15444 TRV130 HCl (Oliceridine) A15972 Naloxegol Oxalate A16155 Docusate Sodium Metabotropic glutamate receptors (mglur) A10006 A10544 A11126 A11181 A11484 (-)-Huperzine A LY (LY404039) BINA ADX LY A11754 VU A11968 CTEP A12139 VU A12467 VU A12498 A12589 Perampanel MPEP hydrochloride A12664 VU A12705 A12909 PHCCC JNJ A13123 LY A13236 MPEP HCl Endocrinology, 2014, 155(7), YIL 781 purchased from Adooq YIL 781 is a ghrelin receptor antagonist (GHS-R1a) (Ki = 17 nm). Available package size: 10,25,50,100mg A12158 BIIE 0246 A12350 Ozarelix A12646 Melanotan II A12790 Parathyroid Hormone 1-34, Human A12860 THIQ Smoothened Receptors A10520 CXCR LDE225 (NVP-LDE225) LDE225 (NVP-LDE225) is a potent, selective and orally bioavailable Smoothened (SMO) antagonist that inhibits hedgehog (Hh) signaling pathway via antagonism of the Smoothened receptor (SMO). Available package size: 5,10,50,100mg Detailed product information is on Page 59. G Protein A11228 QS 11 A11373 CCG Oncogene Sep 28; 36(39): LDE225 (NVP-LDE225) purchased from Adooq A11301 A11492 A11564 A13216 A13779 A14369 A14894 A14944 A15007 A15912 LPA Receptor A10501 A11966 A13981 A13982 A14180 Ki16425 Ki16198 AM095 AM966 AM095 free base A15343 GRI Prostanoid Receptors A11483 A11497 A11742 A12894 Ambrisentan functions as an endothelin receptor antagonist, and is selective for the type A endothelin receptor (ETA). Available package size: 5,10,25,50mg Avosentan (SPP301) Macitentan Sitaxsentan sodium (TBC-11251) RO Atrasentan BQ-788 Endothelin-2, human Bosentan Hydrate Atrasentan HCl BQ-123 Laropiprant (MK0524) MK-2894 Ozagrel hydrochloride PF A11560 SYN-115 (Tozadenant) A11619 CGS HCl A12695 SCH A12846 Tamsulosin hydrochloride A13504 Preladenant A13517 ZM A13745 CVT 6883 A Iodotubercidin A14159 Capadenoson A14327 CGS A14345 IB-MECA IB-MECA has been shown to act as a potent and selective Adenosine A3-R agonist with Ki values of 1.1, 54 and 56 nm for Adenosine A3-R, Adenosine A1-R and Adenosine A2A-R, respectively. Available package size: 5,10,25mg A14402 A15886 A16104 A16105 A16441 CF-102 SCH58261 DPCPX 2-Chloroadenosine (CADO) CGS HCl Cannabinoid Receptors A11096 UR-144 A11253 GW842166X A11513 Org A11547 Rimonabant (SR141716) A11780 JWH 133 A11932 WIN 55,212-2 mesylate Nat Commun. 2016; 7: IB-MECA purchased from Adooq

38 67 GPCR / G Protein GPCR / G Protein 68 A11938 BML-190 A11939 MDA 19 A11942 CP HCl (Otenabant HCl) A12849 AB-FUBINACA A12914 AM251 A14110 PB-22 A14165 JWH 250 A14166 JWH 370 A14167 JWH 073 A14168 JWH 018 A14169 JWH 249 A14170 JWH 307 A14174 AM 2201 A14189 Tedalinab A14993 AM630 A15200 Otenabant A16328 Bay A16397 AM1241 Neurotensin Receptors A11770 SR A13570 ML314 A16026 JMV Orexin Receptors A11500 MK-4305 (Suvorexant) A11567 SB A12503 Almorexant A12633 MK-3697 A12651 SB A12786 SB A13439 TCS 1102 A13778 ACT A14104 JNJ A14286 Almorexant HCl A15231 SB HCl A15233 SB A15982 MDK-5220 A16360 MK-1064 A16396 Alverine Citrate Somatostatin Receptors A12782 Octreotide A13453 Somatostatin A13714 CYN Neurokinin Receptors A10083 Aprepitant (MK-0869) A11069 Fosaprepitant dimeglumine A11756 MK-0517 (Fosaprepitant) A12793 Vofopitant (GR ) A13103 Protease-Activated Receptors (PAR) A12832 Vorapaxar (SCH ) S1P Receptor A10408 A12614 A12906 FTY720 (Fingolimod) ABC CGRP Receptor GW (Casopitant) A13104 Ibodutant (MEN 15596) A13680 A13861 A14428 A15187 A15230 A15254 A15255 Rolapitant GR Netupitant NKP608 SB Talnetant Talnetant hydrochloride Vorapaxar (SCH ) is a potent and orally active thrombin receptor (PAR-1) antagonist with Ki of 8.1 nm. Available package size: 5,10,25,50mg A13495 ML 161 A13039 BAF312 (Siponimod) PF-543 J Infect Dis Dec 15; 214(12): Vorapaxar (SCH ) purchased from Adooq J Neuroinflammation. 2016; BAF312 (Siponimod)purchased from Adooq BAF312 is a next-generation potent sphingosine 1-phosphate (S1P) receptor agonist, selective for S1P1 and S1P5. Available package size: 2,5,10mg PF-543 is a novel selective SK-1 inhibitor which inhibited SK-1 activity in a competitive manner with sphingosine. Available package size: 10,25,50mg A13307 A13637 A15210 A15819 A15833 A15988 A16288 A16289 A16290 Ponesimod CYM 5442 HCl PF-543 Citrate RPC1063 (Ozanimod) NS13001 SKI-II K145 K145 hydrochloride MP-A08 A10598 A11255 A13102 A15165 MK 3207 HCl MK-0974 (Telcagepant) BMS MK-3207 Vasopressin Receptor A11594 A12351 A15784 Tolvaptan Desmopressin OPC21268 A16188 Vasopressin antagonist 1867 Sigma receptor A12479 A12504 Guanylate Cyclase Siramesine Hydrochloride S1RA S1RA is a selective sigma-1 receptor antagonist, with a reported binding affinity of Ki = 17.0 ± 7.0 nm, selective over the sigma-2 receptor and against a panel of other 170 receptors, enzymes, transporters and ion channels. Available package size: 5,10,25,50mg A13036 Siramesine A13196 BD HBr A13513 UMB24 A11549 Riociguat (BAY ) A12402 YC-1 (Lificiguat) A13834 Linaclotide A15891 BAY NF-κB Proc Natl Acad Sci U S A Aug 1; 114(31): S1RA purchased from Adooq The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name NF-κB Other (-)-DHMEQ (+)-DHMEQ Andrographolide Caffeic Acid Phenethyl Ester CID IC50< 0.1 μm JSH-23 IC50: 7.1 μm Parthenolide p53,mdm2 ubiquitination,hdac1 Pyrrolidinedithiocarbamate ammonium QNZ (EVP4593) IC50: 11 nm TNF-α SC75741 EC50: 200 nm A10077 Andrographolide camp A14233 A14266 A14941 A16060 A16116 GHSR A12345 A12346 A14350 A15000 Anamorelin HCl Anamorelin Capromorelin Anamorelin Fumarate Bombesin Receptors A13488 Bombesin Imidazoline Receptor A10232 A10794 A11741 A13409 A13635 A13987 A14256 CCK A11769 A13671 A13713 A15984 NF-κB/IkB A10698 A12748 ESI-09 HJC0350 Bithionol camps-sp, triethylammonium salt SQ22536 Clonidine hydrochloride Rilmenidine Moxonidine HCl Idazoxan Hydrochloride Guanabenz acetate KU14R Rilmenidine Phosphate Loxiglumide (CR1505) Z-360 calcium salt (Nastorazepide calcium salt) Proglumide sodium salt Nastorazepide (Z-360) Parthenolide ((-)-Parthenolide) QNZ (EVP4593) Sci Rep. 2017; QNZ (EVP4593) purchased from Adooq QNZ inhibits the activation of the transcription factor NF-κB and has been used to investigate NF-κB signaling. Available package size: 5,10,25,50mg A13698 Caffeic Acid Phenethyl Ester A14142 JSH 23 Sci Rep. 2018; 8: 487. JSH 23 purchased from Adooq JSH 23 is an inhibitor of NF-κB, blocking its translocation into the nucleus with IC50 value of 7.1 um. Available package size: 5,10,25mg

39 69 NF-κB/IkB TGF-β / Smad 70 A14278 A14809 A15046 A16233 A16301 A16302 A16303 A16304 A16306 IKK/IκB The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name IκB IKK Other AZD3264 Bardoxolone Methyl NF-κB,Nrf2 BAY IC50: 10 μm Bay IC50: 10 μm Bay IC50: 10 μm BMS BMS HCl BX-795 IKK2, IC50: 0.3 μm; IKK1, IC50: 4 μm IKK2, IC50: 0.3 μm; IKK1, IC50: 4 μm IKK-16 IKK2, IC50: 40 nm; IKK1, IC50: 200 nm; IKK complex, IC50: 70 nm IMD 0354 LY IKK2, IC50: 30 nm MLN120B IKKβ IC50: 20 μm MRT67307 IKKϵ IC50: 160 nm TBK1 PHA 408 SC75741 Dehydrocostus Lactone CID Tomatidine (+)-DHMEQ (-)-DHMEQ Adjudin Didox Pyrrolidinedithiocarbamate ammonium IKK2 IC50: 40 nm PS-1145 IC50: 88 nm SC-514 IC50: 3-12 μm TPCA-1 IKK2, IC50: 17.9 nm WS3 EBP1 WS6 EBP1 A11148 BX-795 A11318 BMS HCl A11323 Bardoxolone methyl (RTA 402) A11324 Bardoxolone (CDDO) A11338 Bay HCl TGF-β / Smad Inhibitors A10449 Hesperetin A10826 SB A10827 SB A11017 LY E2-conjugating enzymes PDK-1,c-Kit, CDK2/CyclinE CDK2/CyclinA, AUR2, PRAK Am J Physiol Heart Circ Physiol Nov 1;307(9): H LY purchased from Adooq Available package size: 5,10,25,100mg Bardoxolone methyl is an orally-available first-in-class synthetic triterpenoid. It is an inducer of the Nrf2 pathway, which can suppress oxidative stress and inflammation. Available package size: 25,50,100,200mg A11339 Bay A11452 IKK-2 inhibitor VIII A11463 IKK-3 Inhibitor A11485 MRT67307 A11579 TPCA-1 A11957 Bay A12470 BAY A12559 BMS A12746 SC-514 A12789 PS-1145 A12836 IKK-16 A12837 IMD 0354 A12952 WS3 A12953 WS6 A13108 PHA 408 A13537 BI A14804 Wedelolactone A15018 Bay R form A15171 MLN120B A15488 LY A15900 AZD3264 A16297 Amlexanox A16298 IKK epsilon-in-1 A16299 CDDO-EA HDAC TGF-β / Smad Neurobiology of disease, 2016, 89: Bardoxolone methyl (RTA 402) purchased from Adooq Detailed product information is on Page 1. A11083 A11133 GW LY Proc Natl Acad Sci U S A Oct 25; 113(43): LY purchased from Adooq LY , a novel transforming growth factor β receptor type I and type II dual inhibitor, as a therapeutic approach to suppressing pancreatic cancer metastasis Available package size: 5,10,50,100mg A11157 SB The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name ALK1 ALK2 ALK3 ALK4 TGFβRI/ALK5 ALK6 ALK7 TGFβRII TGF-β Smad3 Other A IC50: 25 nm A DMH1 EW-7197 Galunisertib GW IC50: nm IC50: 12 nm IC50: 13 nm IC50: 45 nm IC50: 11 nm IC50: 56 nm IC50: 18 nm IC50: 7.5 nm Hesperetin Histamine receptor ITD 1 IC50: 0.85 μm K02288 LDN LDN HCl LDN LDN LY LY ML347 Pirfenidone R RepSox SB SB SB SD-208 SIS3 A11205 IC50: 1.8 nm IC50: 1.1 nm IC50: 5 nm IC50: 5 nm IC50: 2.4 nm IC50: 1.3 nm IC50: 24 nm IC50: 46 nm LDN IC50: 32 nm IC50: 34.4 nm IC50: 302 nm IC50: 321 nm IC50: 30 nm IC50: 30 nm IC50: 85.8 nm IC50: 2133 nm IC50: 9276 nm IC50: 10.8 μm Ki: 38 nm IC50: 59 nm IC50: 2.5 nm IC50: 4 nm IC50: 94 nm IC50: 129 nm IC50: 47 nm IC50: 14.3 nm IC50: 48 nm Int J Mol Med May; 35(5): LDN purchased from Adooq LDN is a highly potent small molecule BMP inhibitor that inhibits BMP type I receptors ALK2 (IC50: 5 nm), ALK3 (IC50: 30 nm) and ALK6 (TGFβ1/BMP signaling) and subsequent SMAD phosphorylation. Available package size: 2,5,25,50mg A11478 LDN HCl A11762 RepSox (SJN 2511) A12358 A A12820 DMH-1 A12821 LDN A12924 ITD-1 A12926 Kartogenin A13446 LY A14066 SD-208 A14213 EW-7197 A14298 ML347 A14311 K02288 A14436 A A14810 Alantolactone A15185 NG25 IC50: 6.4 nm IC50: 9.83 μm Ki: 300 nm IC50: 0.4 μm A15232 SB HCl A16065 SIS3 A16073 (+)-ITD 1 A16096 LDN A16207 R A16208 Chebulinic acid A16209 Pirfenidone A16210 SRI hydrochloride Protein Kinase C (PKC) A10196 Chelerythrine Chloride A10261 Bryostatin 1 A10286 Daphnetin A10356 LY (Enzastaurin) RIPK2,CK1δ, MLK-7K LY (Enzastaurin) is a potent and selective inhibitor of PKCβ with antiproliferative activity (IC50= ~6 nm). Available package size: 10,50,100,200mg A10616 A10766 A10864 A12014 A12399 Myricitrin (Myricitrine) Quercetin (Sophoretin) Staurosporine Verbascoside Ruboxistaurin (LY333531)

40 71 TGF-β / Smad TGF-β / Smad 72 The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name PKC PKCα PKCβ PKCγ PKCδ PKCε PKCζ PKCη PKCθ PKCμ Other Bisindolylmaleimide I Bryostatin 1 Chelerythrine chloride Daphnetin Enzastaurin Go 6983 Go6976 Midostaurin Myricitrin PKC (19-36) Quercetin Ro Mesylate Ruboxistaurin (LY333531) Sotrastaurin Staurosporine A11554 IC50: 20 nm Ki: 1.35 nm IC50: 660 nm IC50: μm IC50: 39 nm IC50: 7 nm IC50: 7.9 nm IC50: 0.18 um IC50: 22 nm IC50: 5 nm IC50: 17 nm IC50: 6 nm IC50: 7 nm IC50: 6.2 nm IC50: 30 nm IC50: 2.3 nm IC50: 24 nm IC50: 0.36 μm Ki: 0.95 nm IC50: 2 nm Sotrastaurin (AEB071) A12419 Go 6976 A12650 PKC 412 (Midostaurin) IC50: 20 nm IC50: 83 nm IC50: 6 nm IC50: 10 nm IC50: 110 nm IC50: 60 nm IC50: 24 nm IC50: 330 nm IC50: 1.25 μm IC50: 465 μm IC50: 160 nm IC50: 27 nm PKCβ1, IC50: 4.7 nm; PKCβ2, IC50: 45.9 nm; IC50: 0.3 μm Ki: 0.64 nm Sotrastaurin is a protein kinase C inhibitor for the prevention of transplant rejection and treatment of psoriasis Available package size: 5,10,25,50mg IC50: 0.25 μm Ki: 2.1 nm IC50: 5 nm IC50: 20 nm PKC 412 is a broad spectrum protein kinase inhibitor. Inhibits conventional PKC isoforms α/β/γ, PDFRβ, VEGFR2, Syk, Flk-1, Flt3, Cdk1/B, PKA, c-kit, c-fgr, c-src, VEGFR1 and EGFR. Displays potent antitumor activity. Available package size: 5,10,25,50mg A12963 Ingenol Mebutate (PEP005) A13043 (-)-Indolactam V A13094 alpha-amyloid Precursor Protein Modulator A13197 GF X A13514 Ro A13679 Prostratin A13790 GO6983 A14307 NH125 A14336 Valrubicin A O-tetradecanoyl phorbol-13-acetate A14871 PKC (19-36) A14882 [Ser25] Protein Kinase C (19-31) A15557 TAS 301 A16212 PKC-IN-1 A16213 NSC IC50: 24 nm Ki: 3.2 nm IC50: 73 nm IC50: μm Ki: 1.8 nm IC50: 1086 nm IC50: 4 nm Protein Kinase A (PKA) A10286 Daphnetin A11034 A A11935 H 89 2HCl Ki: 0.22 nm IC50: 20 μm A12464 AT13148 A13584 A-3 Hydrochloride A14307 NH125 A14868 PKA inhibitor fragment (6-22) amide A15006 AT7867 2HCl A Bromo-cAMP A15914 Dibutyryl-cAMP A16016 KT 5720 A Bnz-cAMP sodium salt A16028 camps-rp, triethylammonium salt A16031 PKI amide, myristoylated A16052 cgmp Dependent Kinase Inhibitor Peptid A16189 CCG A16222 Synaptamide PDGFR EGFR, PKA FLT3, JAK2 PPK,KDR, c-syk Sirtuin,Src, PI3Kγ c-fgr, S6 kinase Biochemical and biophysical research communications, 2016, 472(4), A purchased from Adooq A is a B/Akt inhibitor with an IC50 of 14 nm and also shows inhibitory activity against PKA and CDK2 with IC50 of 16 and 46 nm, respectively. Available package size: 5,10,25,50mg Oncogene (2017), 1 12 H 89 2HCl purchased from Adooq H 89 dihydrochloride is a cell-permeable, selective, reversible, ATP-competitive and potent inhibitor of protein kinase. Available package size: 10,25,50,100mg ROCK A10381 A10441 A10928 A11001 Fasudil HCl (HA-1077) GSK429286A Thiazovivin Y HCl Scientific Reports, 2017, 7:42186 Y HCl purchased from Adooq Y is a Rho-Associated Coil Kinase (ROCK) inhibitor that increases the cloning efficiency of human embryonic stem cells (hescs). Available package size: 5,10,25,50mg A11610 Y A12348 GSK A12464 AT13148 A12674 SR 3677 dihydrochloride A13659 Glycyl-H HCl A13785 HA-1077 dihydrochloride A13067 RKI-1447 RKI-1447 is a potent inhibitor of the Rho-associated ROCK kinases with anti-invasive and antitumor activities in breast cancer. Available package size: 5,10,25,50mg A15045 chroman 1 A15101 H-1152 A15102 H-1152 dihydrochloride A15118 Hydroxyfasudil A15119 Hydroxyfasudil hydrochloride A15178 Narciclasine A15225 ROCK inhibitor A15226 ROCK inhibitor-1 A15239 SLx-2119 (KD025) A15888 Ripasudil A15921 SAR HCl A16211 LX7101 Neuronal Signaling β-amyloid A14075 Amyloid b-peptide (1-42) (human) A15414 Amyloid b-peptide (42-1) (human) The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do A15415 A15416 A15417 Amyloid b-peptide (10-20) (human) Amyloid b-peptide (25-35) (human) Amyloid b-peptide (12-28) (human) Inhibitor Name Beta Amyloid Other Avagacestat IC50: 0.3 nm A15418 Amyloid b-peptide (1-40) (human) DAPT (GSI-IX) IC50: 20 nm A15419 Amyloid b-peptide (1-40) (rat) LY EC50: ~300 nm BACE1 A15420 Amyloid b-peptide (1-42) (rat) MK-0752 IC50: 5 nm A15421 Amyloid b-peptide (1-43) (human) RO IC50: 14 nm γ secretase,γ secretase(icn) A15423 beta-amyloid (1-11) A10157 BMS (Avagacestat) A15424 Amyloid b-protein (1-15) A10312 Dimebon 2HCl A10802 RO γ-secretase A11194 MK-0752 RO is an orally bioavailable, small-molecule gamma secretase (GS) inhibitor with an IC50 of 4 nm. Available package size: 5,10,50,200mg MK-0752 inhibits the Notch signaling pathway, which may result in induction of growth arrest and apoptosis in tumor cells in which the Notch signaling pathway is overactivated. Available package size: 5,10,50,100mg A11776 LY A12647 Ro A13094 alpha-amyloid Precursor Protein Modulator A10157 A10288 BMS (Avagacestat) DAPT (GSI-IX) DAPT (GSI-IX) is an inhibitor of γ-secretase that causes a reduction in Aβ40 and Aβ42 levels in human primary neuronal cultures with IC50 values of 115 and 200 nm for total Aβ and Aβ42 respectively. Available package size: 5,10,50,100mg A10802 RO A10836 Semagacestat (LY450139) Oncogene Mar; 36(11): Semagacestat (LY450139) purchased from Adooq Available package size: 5,10,50,100mg

41 73 Neuronal Signaling Neuronal Signaling 74 The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Beta-secretase (BACE) A13932 A14004 Cloflubicyne Picrotoxin CaMK Inhibitor Name γ secretase Aβ Notch Other Avagacestat IC50: 0.3 nm Begacestat (GSI-953) BMS CHF5074 Aβ42, EC50: 12.4 nm; Aβ40 EC50: 14.8 nm IC50: 12 nm Aβ42, EC50: 3.6 μm; Aβ40 EC50: 18.4 μm DAPT (GSI-IX) IC50: 20 nm Dibenzazepine IC50: 2.6 nm IC50: 2.9 nm FLI-06 EC50: 2.3 μm IMR-1 IC50: 6 μm IMR-1A IC50: 6 μm JLK 6 IC50: ~30 μm L Ki: 17 nm LY Notch-1 IC50: 1nM LY IC50: nm IC50: 0.39 nm A10543 LY British Journal of Pharmacology, 2016, 174(5) LY purchased from Adooq LY is a novel potent agent that is used to treat Alzheimer's Disease in preclinical experiments. Available package size: 5,10,50,100mg A11776 LY Nat Commun Oct 11;7: LY purchased from Adooq A14005 Muscimol A14281 Oxiracetam A14343 a5ia A14349 RO A Aminobutyric acid A15083 Etifoxine A15084 Etifoxine hydrochloride A15277 Vigabatrin A15288 Zolpidem A15441 Vigabatrin A15939 CTP354 A16135 Tiagabine hydrochloride A16171 Piperazine The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name CaMKII CaMKIII CaMKKα CaMKKβ Other A IC50: 0.28 μm CID KN-62 Ki: 0.9 μm KN-93 Phosphate Ki: 0.37 μm NH125 IC50: 60 nm STO-609 acetate A10719 A11473 IC50: 40.5 μm Ki: 0.25 μm Ki: 47 nm Phenoxybenzamine hydrochloride KN-62 PKD1, PKD2, PKD3, PKC, CAK, PLK1, Akt PKC,PKA MK-0752 IC50: 5 nm Aβ40 MRK 560 IC50: 0.65 nm A16336 U PF IC50: 6.2 nm RO IC50: 4 nm IC50: 5 nm Aβ40 Semagacestat IC50: 10.9 nm IC50: 14.1 nm TC-E 5006 Aβ42, EC50: 390 nm Z-Ile-Leualdehyde A11174 A11176 YO LY LY is the first orally available non-peptidic BACE1 inhibitor that produces profound Aβ-lowering effects in animals. Available package size: 5,10,50,100mg A12825 AZD3839 A13249 AZD5423 A14407 AMG-8718 A14591 Timosaponin b-ii NMDA Receptors A10251 Flupirtine maleate A11708 Memantine hydrochloride A11712 Orphenadrine citrate A11862 Felbamate A11947 TCN 201 KN-62 is a selective, cell-permeable inhibitor of CaM kinase II. Available package size: 5,10,25mg A12416 CID A12423 kb NB A13276 KN-93 A16113 Verubecestat (MK-8931) Scientific Reports 7, KN-93 Maleate purchased LY is a selective, cell permeable, small molecule gamma secretase inhibitor. Available package size: 5,10,50,100mg A11194 MK-0752 A11258 Begacestat (GSI-953) A11259 PF A11337 BMS A11393 E 2012 A11425 gamma-secretase modulator 1 A11427 gamma-secretase modulator 2 A11776 LY A12433 Flurizan A12444 BMS A13217 TC-E 5006 A13319 PF A13544 LY A13662 Flurbiprofen Axetil A13815 FLI-06 A14088 LY A15090 gamma-secretase modulator 3 A15296 Compound W A15301 JLK 6 A15304 MRK 560 A15899 L A16152 IMR-1 A16214 CHF5074 A16215 Z-Ile-Leu-aldehyde A16223 IMR-1A COX Detailed product information is on Page 60. GABA Receptors A10121 A10252 A10397 A10412 A10413 A10414 A10631 A10754 A10849 A12298 A12590 A12689 A12993 A13198 A13449 A13459 A13613 A13696 Baicalin Dihydromyricetin (Ampeloptin) Flumazenil Furosemide Gabapentin Gabapentin Hydrochloride Nefiracetam (Translon) Primidone (Mysoline) SKF 89976A HCl Bemegride (+)-Bicuculline Phenazepam Zaleplon Tiagabine Lorediplon Muscimol hydrobromide Guvacine hydrochloride 2-Hydroxysaclofen A13726 AWD A13769 A13784 Indiplon Bretazenil TCN 201 is a NMDA receptor antagonist selective for NR1/NR2A over NR1/NR2B-containing receptors. Available package size: 10,25,50,100mg A12426 SDZ A12751 NMDA A12761 (+)-MK 801 Maleate Scientific Reportsvolume 7, 3575 (+)-MK 801 Maleate purchased from Adooq (+)-MK 801 is a potent antagonist of NMDA with Ki value of 30.5nM. Available package size: 10,25,50mg A12946 Eliprodil A13435 (-)-MK 801 maleate A13576 GLYX-13 (Rapastinel) A13729 MDL A13858 ARL A14006 Ibotenic Acid A14071 NVP-AAM077 Tetrasodium Hydrate (PEAQX) A15235 SDZ Ammonium salt A15522 L A15523 CIQ A15791 CGS19755 A16083 RO maleate A16109 CNQX from Adooq KN-93 is an inhibitor of multifunctional Ca++/calmodulin-dependent protein kinase. Available package size: 5,10,25mg A13447 A A13804 CID A13809 CID A13897 K252a A14288 KN-93 Phosphate A14307 NH125 A15137 KN-92 A15138 KN-92 hydrochloride A15139 KN-92 phosphate A16318 CRT A16345 STO-609 acetate AChR A10098 A10147 A10180 A10330 A10386 A10416 A10417 A10476 A10480 A10579 Atropine Biperiden HCl Bethanechol chloride Donepezil hydrochloride Fesoterodine fumarate (Toviaz) Galanthamine hydrobromide Gallamine triethiodide Ipratropium bromide Irsogladine Methscopolamine bromide

42 75 Neuronal Signaling Proteases 76 A10635 Neostigmine bromide (Prostigmin) A10684 Oxybutynin A10803 Rocuronium bromide A10808 SVT (Tarafenacin) A10937 Tolterodine tartrate (Detrol LA) A10966 Varenicline A hydroxymethyl tolterodine (PNU ) A11203 PNU A11215 Solifenacin succinate A11233 PNU A11290 A A11545 Metanicotine A11706 Tropicamide A11712 Orphenadrine citrate A11716 Adiphenine HCl A11719 Rivastigmine tartrate A11975 Methoctramine hydrate A11987 Darifenacin A12161 Catharanthine sulfate A12641 Glycopyrrolate A12681 Methyllycaconitine citrate A12835 MK7622 A12900 Flavoxate A13071 Arecoline A13539 A A13548 PF A Iodo-A HCl A13653 Benzethonium Chloride A13685 Xanomeline oxalate A13688 ABT-418 HCl A13761 (-)-Nicotine ditartrate A13842 Sofinicline (ABT-894, A ) A13856 AF-DX 384 A13925 Deoxyvasicine HCl A14096 Rivastigmine A14183 Ispronicline (TC-1734, AZD-3480) A14205 TBPB A14217 LY A14229 Nitenpyram A14244 Diphenidol HCl A14353 Pulegone A14375 Tropisetron HCL A15042 Cevimeline hydrochloride hemihydrate A15086 EVP-6124 (Encenicline) A15087 EVP-6124 hydrochloride A15268 Umeclidinium bromide A15490 Imidafenacin A15782 Acotiamide hydrochloride trihydrate A15950 GTS-21 (DMBX-A) A15986 Revefenacin A16390 Acetylcholine iodide P2X Receptor A11107 GW HCl A11316 A A is a novel competitive antagonist of P2X7 receptors (IC50 values = 40 nm for human and 18 nm for rat). Available package size: 10,25,50,100mg A11690 Ticlopidine HCl A11972 NF 279 A12412 A sodium salt hydrate A13131 AF-353 A14983 A hydrochloride A16066 A A is a P2X7 selective, competitive antagonist with the IC50s value for human, rat and mouse channels of 11, 10 and 9 nm, respectively. Available package size: 5,10,25mg Purinergic (P2Y) Receptors A10233 A10748 A11238 A11486 MRS 2578 GlyT A15021 A15022 A16406 Clopidogrel (Plavix) Prasugrel (Effient) Ticagrelor (AZD6140) Ticagrelor (AZD6140) is the first reversibly binding oral P2Y(12) receptor antagonist that blocks ADP-induced platelet aggregation. Available package size: 25,50mg A15443 A16106 A16144 MRS 2578 is a selective antagonist of P2Y6 nucleotide receptors. Available package size: 10,25,50,100mg AZD1283 Methylthioadenosine Prasugrel Hydrochloride Bitopertin Bitopertin (R enantiomer) Amoxapine Caspase Detailed product information is on Page 10. γ-secretase Detailed product information is on Page 72. Proteasome The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name Proteasome 20S proteasome Bortezomib (PS-341) Ki: 0.6 nm Carfilzomib (PR-171) IC50: 5 nm Celastrol IC50: 2.5 μm Delanzomib (CEP-18770) IC50: 3.8 nm Epoxomicin Ixazomib (MLN2238) Ki: 0.93 nm MG-132 IC50: 100 nm MLN9708 Ki: 0.93 nm ONX-0914 (PR-957) IC50: ~10 nm Oprozomib (ONX 0912) IC50: 36 nm PI-1840 IC50: 27 nm VR23 IC50: 1 nm A10160 Bortezomib (Velcade) Nat Chem Biol Sep; 11(9) Bortezomib (Velcade) purchased from Adooq Bortezomib is a highly selective, reversible inhibitor of the 26S proteasome. Available package size: 10,25,50,100mg A10600 MLN2238 A10602 MLN9708 A11043 MG-132 Proteases Int J Mol Sci Jan; 18(1): 44. MG-132 purchased from Adooq MG-132 is a potent cell-permeable inhibitor of proteasome (IC50 = 100 nm) and calpain (IC50 = 1.2 μm). Available package size: 10,25,50,100mg A11145 CEP A11278 PR-171 (Carfilzomib) A11601 MG-115 A12220 MG-262 A12653 ONX-0914 Sci Rep. 2016; 6: ONX-0914 purchased from Adooq Available package size: 5,10,25,50mg A12730 Epoxomicin A12768 Lactacystin A13650 VR23 A13711 Gliotoxin A13853 Marizomib (NPI-0052, salinosporamide A) A14048 PSI A14146 PI-1840 A14181 ONX 0912 (Oprozomib) A14910 Aclacinomycin A A14922 AM 114 A14932 Dihydroeponemycin A15427 Clasto-Lactacystin b-lactone HCV Protease The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name HCV Protease Anguizole NS4B, IC50: 310 nm Asunaprevir (BMS ) NS3, IC50: 1 nm Boceprevir (SCH ) Ki: 14 nm Ciluprevir (BILN 2061) NS3, IC50: 3 nm Daclatasvir (BMS ) EC50: 9-50 pm Danoprevir (ITMN-191) IC50: nm Ledipasvir (GS5885) Lomibuvir (VX-222, VCH-222) IC50: 0.94 μm Simeprevir NS3/4A, Ki: 0.36 nm Telaprevir (VX-950) IC50: 0.35 μm A10159 A10284 A10902 BMS Danoprevir (RG7227) Telaprevir (VX-950) Antimicrob Agents Chemother Nov; 60(11): Telaprevir (VX-950) purchased from Adooq Telaprevir (VX-950) is known as protease inhibitors that inhibits the hepatitis C virus NS3.4A serine protease. Available package size: 2,5,10,25mg A10980 VX-222 A11294 Anguizole Virus genes, 2013, 47(3), Anguizole purchased from Adooq Anguizole is a small molecule inhibits HCV replication and alters NS4B's subcellular distribution. Available package size: 5,10,25,50mg A11295 Asunaprevir (BMS ) Antimicrob Agents Chemother Aug; 58(8): Asunaprevir (BMS ) purchased from Adooq Available package size: 5,10,25,50mg

43 77 Proteases Proteases 78 A11332 A10096 A10097 Boceprevir (SCH ) Boceprevir is a protease inhibitor used as a treatment for hepatitis C genotype 1. Available package size: 5,10,25,50mg A11335 Balapiravir (R1626) A11336 BMS HCl A11343 Ciluprevir (BILN 2061) A11506 Narlaprevir A11510 Nesbuvir A11519 PSI-6130 A11529 PSI-7977 A11530 PSI-6206 A11580 Simeprevir A11583 Tegobuvir (GS-9190) A11600 Vaniprevir A12374 VCH-916 A13105 Setrobuvir (ANA-598) A13118 Celgosivir A13155 Ledipasvir (GS 5885) A13414 A13526 A13787 A13965 A14046 A14106 A15166 A15167 A15168 A15224 A15479 HIV Protease Atazanavir sulfate (BMS ) Atazanavir Hepatology Nov;60(5): Boceprevir (SCH ) purchased from Adooq Sci Rep. 2016; 6: Ledipasvir (GS 5885) purchased from Adooq Ledipasvir is an inhibitor of the hepatitis C virus HCV NS5A protein. Available package size: 5,10,25,50mg BI (Deleobuvir) GS-9256 MK-5172 MK 8742 (elbasvir) GS-9451 Faldaprevir MK-5172 hydrate MK-5172 potassium salt MK-5172 sodium salt RO-9187 VCH-759 Atazanavir is an antiretroviral drug of the protease inhibitor (PI) class. Like other antiretrovirals, it is used to treat infection of human immunodeficiency virus (HIV). Available package size: 5,10,25,50mg A10537 DPP-4 The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name Alogliptin IC50: <10 nm Linagliptin IC50: 1 nm Saxagliptin IC50: 26 nm Sitagliptin phosphate monohydrate IC50: 19 nm Trelagliptin Vildagliptin (LAF-237) IC50: 2.3 nm A10848 A11109 A11224 A12528 A13310 A13311 A13312 A13529 A13571 A14293 A14377 A15258 A15298 A15309 A15320 Lopinavir (ABT-378) Sitagliptin phosphate monohydrate Saxagliptin (BMS ) Linagliptin (BI-1356) Vildagliptin MK-3102 Alogliptin Benzoate Trelagliptin Succinate (SYR-472) Anagliptin Alogliptin Trelagliptin Sitagliptin Teneligliptin hydrobromide DPPI 1c hydrochloride PK 44 phosphate Scientific Reports volume 6, Lopinavir (ABT-378) purchased from Adooq Available package size: 10,100,200mg A10799 Ritonavir A11201 BMS-806 (BMS ) A11378 Saquinavir A11504 Nelfinavir A11853 Darunavir Ethanolate (Prezista) A11871 Indinavir sulfate A11985 Amprenavir A12583 Fosamprenavir A13156 GSK A A13199 Trovirdine A14148 BMS A14194 Bevirimat A14259 Nelfinavir Mesylate A14262 Pepstatin A A15025 BMS (Fostemsavir) A15026 BMS Tris A15089 Fosamprenavir Calcium Salt A15262 Tipranavir A15825 Enfuvirtide Acetate(T-20) A15965 GSK A16024 (±)-BI-D NVP DPP 728 dihydrochloride DPP-4 A15505 A16047 Cysteine protease The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Aloxistatin Inhibitor Name Cysteine Protease Other Calpeptin ID50: 52 nm Cathepsin Inhibitor 1 pic50: 5.2 E-64 IC50: 9 nm Leupeptin Hemisulfate serine protease Loxistatin Acid (E-64C) MG-101 (ALLN) Odanacatib (MK-0822) IC50: 0.2 nm PD IC50: 5.33 μm PMSF chymotrypsin Z-FA-FMK A11265 Odanacatib (MK-0822) A11466 Cathepsin Inhibitor 1 A11901 A12020 A13256 PMSF Balicatib CA-074 A13257 E-64 A13258 A13259 A13502 A13593 A13611 A13640 A14145 A14220 Loxistatin Acid (E64-C) E 64d (Aloxistatin) Z-FL-COCHO CA-074 Methyl Ester Gly-Phe-beta-naphthylamide SJA6017 Leupeptin hemisulfate MG-101 A14245 PD A14284 A14911 A15290 A15295 Teneligliptin UAMC dihydrochloride Z-FA-FMK Calpain Inhibitor II, ALLM Acetyl-Calpastatin ( ) (human) Calpeptin A15302 L A15303 MDL A15306 PD A15313 SID A16381 Z-FA-FMK Calpeptin is a cell permeable calpain inhibitor. Available package size: 10,25,50mg Z-FA-FMK is an irreversible inhibitor of cysteine protease. Available package size: 1,2,5mg Serine Protease The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name Serine Protease Other AEBSF HCl Alvelestat (AZD9668) IC50: 12 nm Aprotinin Ki: 9.5 nm Thrombin,Trypsin,kallikrein Leupeptin Hemisulfate Cysteine protease Nafamostat Mesylate PMSF cysteine protease A10617 Aminopeptidase A10208 A13592 A15299 Thrombin Nafamostat mesylate A11325 BCX 1470 methanesulfonate A11331 BCX 1470 A11764 Camostat mesylate A11901 PMSF A12779 Alvelestat A13605 AAF-CMK A14073 Sivelestat sodium salt A14145 Leupeptin hemisulfate A14184 Sivelestat A14263 Aprotinin A14270 AEBSF HCl A15315 SSR A16137 Sivelestat sodium hydrate CHR2797 (Tosedostat) Bestatin Methyl Ester Fumagillin A10138 BIBR 953 (Dabigatran, Pradaxa) A10139 BIBR-1048 (Dabigatran etexilate) A11774 Argatroban A12509 Ximelagatran A14087 Avatrombopag A15023 Bivalirudin Trifluoroacetate A15057 Dabigatran etexilate mesylate A15058 Dabigatran ethyl ester A15078 Eltrombopag Olamine A16048 PPACK Dihydrochloride A16287 TPO agonist 1 MMP Nafamostat is an anticoagulant. Broad spectrum serine protease inhibitor. Reduces eosinophil infiltration, mast cell activation and airway responsiveness in a murine model of asthma. Available package size: 10,25,50,100mg

44 79 Proteases Microbiology 80 The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do A10745 A11345 A12826 Inhibitor Name Batimastat (BB-94) IC50: 3 nm Ilomastat (GM6001, Galardin) Ki: 3.6 nm Marimastat (BB-2516) IC50: 5 nm Nobiletin NSC Doxycycline HCl CTS-1027 Marimastat SB-3CT Ki: 13.9 nm A12848 A12985 MMP 4-epi-Chlortetracycline Hydrochloride Batimastat (BB-94) Marimastat acted as a broad-spectrum matrix metalloproteinase inhibitor. Available package size: 5,10,25,50mg Batimastat (BB-94) is a potent and synthetic inhibitor of a broad spectrum of matrix metalloproteinases (MMPs), including interstitial collagenase (IC50 = 3 nm), stromelysin (IC50 = 20 nm), Mr 72,000 type IV collagenase (IC50 = 4 nm), Mr 92,000 type IV collagenase (IC50 = 4 nm), and matrilysin (IC50 = 6 nm). It is a low-molecularweight (MW = 478) and peptide-like collagen substrate analogue consisting of a peptide backbone and a hydroxamic acid group which bind to MMPs and the catalytically active zinc atom respectively. Available package size: 5,10,25,50mg A13072 NSC A13320 GM 6001 GM 6001 is a potent, reversible broad spectrum inhibitor of zinccontaining proteases, including matrix metalloproteinases (MMPs). Available package size: 10,25,50mg A13597 CL A13724 TAPI-0 A14009 TAPI-2 A14070 TAPI-1 A14253 SB-3CT A15292 ARP 100 A15293 ARP 101 A15205 ONO 4817 A15307 PD A15311 Ro A15316 UK A15317 WAY A15297 CP CP , broad spectrum MMP inhibitor (IC50 values are 0.7, 0.9, 13, 16 and 1170 nm for MMP-2, MMP-13, MMP-9, MMP-3 and MMP-1 respectively). Available package size: 10,25,50mg A15322 GI X A15323 UK A15326 Batimastat sodium salt A (R)-Ginsenoside Rh2 A15945 Abametapir A16043 DC_AC50 Urokinase A15324 A15325 A16057 Tyrosinase A10058 A10084 A Chlorophenylguanidine hydrochloride BC 11 hydrobromide GGACK Dihydrochloride Aloin (Barbaloin) Arbutin (Uva, p-arbutin) MNS Carboxypeptidases A12809 A15035 A MPPA Carboxypeptidase G2 (CPG2) Inhibitor PMPA A15318 ZJ 43 Glutaminase A14396 Elastases A14073 A14184 A14912 A14913 CB-839 CB-839 an is orally bioavailable inhibitor of glutaminase, with potential antineoplastic activity. Available package size: 5,10,25mg A14954 BPTES Sivelestat sodium salt Sivelestat Elastase Inhibitor A15315 SSR A16137 Elastase Inhibitor, SPCK ONO-5046 sodium hydrate Reverse Transcriptase The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name Reverse Transcriptase Other Abacavir sulfate Adefovir Dipivoxil Dapivirine (TMC120) IC50: 24 nm Didanosine IC50: 490 nm Emtricitabine Entecavir Hydrate Lamivudine Nevirapine Rilpivirine Tenofovir Tenofovir Disoproxil Fumarate Zidovudine A10039 Adefovir dipivoxil A10306 Didanosine A10349 Emtricitabine A10512 Lamivudine A10639 Nevirapine (Viramune) A10908 Tenofovir (Viread) A10909 Tenofovir Disoproxil Fumarate A11115 Abacavir A11120 Abacavir sulfate A11216 Entecavir A11542 Rilpivirine (R , TMC 278) A12443 MK-1439 A12587 Dapivirine A12667 Lersivirine (UK ) A14435 Elvucitabine A15428 Zidovudine A15772 GS-7340 Integrase The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name Integrase BMS IC50: 15 nm Cabotegravir (GSK744, GSK ) Dolutegravir (GSK ) IC50: 2.7 nm Elvitegravir (GS-9137, JTK-303) IC50: nm MK-2048 IC50: nm Raltegravir (MK-0518) IC50: nm A10156 A10347 A10775 A11068 A11135 BMS Elvitegravir (GS-9137) Raltegravir (MK-0518) S/GSK (Dolutegravir) MK-2048 Microbiology A13984 GSK (GSK744) Sodium salt A16014 GSK744 (S/GSK ) A16018 BI A16162 Dolutegravir Sodium HCV Protease Detailed product information is on Page 76. HIV Protease Detailed product information is on Page 77. CCR Detailed product information is on Page 61. Antifection A10072 A10073 A10118 A10189 A10235 A10481 A10496 A10533 A10742 A10933 A10960 A11124 A11139 A11362 A11401 A11422 A11585 A11645 A11653 A11829 A11844 A11893 A11927 A12124 A12459 A12485 A12576 A12998 A13393 A13486 A13543 Amorolfine HCl Amphotericin B Aztreonam (Azactam, Cayston) Cefoselis sulfate Cloxacillin sodium Isoconazole nitrate Kanamycin sulfate Linezolid (PNU ) Polymyxin B sulphate Tigecycline Bacitracin Peramivir Retapamulin (SB ) Calcitetrol PA-824 (Pretomanid) Fiacitabine TMC Ganciclovir Oseltamivir phosphate (Tamiflu) Butenafine HCl Cefradine Naftifine HCl Chlortetracycline Hydrochloride BM212 Moxidectin SQ109 Fusidate Sodium Laninamivir (CS-8958) Sancycline Eperezolid Ganciclovir Mono-O-acetate

45 81 Microbiology Stem Cells / Wnt 82 A13612 A13658 A13697 A13851 A14031 A14228 A14237 A14246 A14254 A14818 A14942 A14965 A14995 A14996 A14999 A15120 A15431 A15599 A15626 A15771 A15788 A15831 A15835 A15909 A15943 A15948 A15993 A15996 A16003 A16004 A16005 A16008 A16011 Hedgehog A10249 A10258 A11048 A11351 DL-cycloserine Quinupristin Cefixime Rolitetracycline Solithromycin Erythromycin Cyclocarbonate Mefloquine HCl Micafungin Sodium Demeclocycline HCl Betamipron Imipenem (S)-Tedizolid Amadacycline Amadacycline methanesulfonate AN-2690 I2906 TBA-354 Bronopol Broxyquinoline Oritavancin (LY333328) Ascomycin (FK520) Rifamycin S Presatovir (GS-5806) Sodium Tauroursodeoxycholate Calicheamicin Dalbavancin HCl VX-787 (Pimodivir) Tildipirosin Dihydrostreptomycin sulfate Chloroxylenol Cefotaxime sodium Nitrofurantoin Furazolidone Cyclopamine GDC-0449 (Vismodegib) LY (Taladegib) TAK-441 A11442 GANT 58 A12418 A12920 A13095 A13252 HhAntag Hh-Ag1.5 SANT-1 GANT61 Available package size: 10,25,50,100mg A16012 A16070 A16072 A16118 A16156 A16157 A16160 A16161 A16163 A16165 A16168 A16382 A16395 A16401 A16403 A16407 A16408 A16421 A16422 A16425 A16429 A16434 A16435 A16457 A16459 A16460 A16461 A16464 A16466 A16467 A16468 A16469 A16473 Stem Cells / Wnt Sci Rep. 2017; 7: GANT61 purchased from Adooq A16111 Wnt Ethylparaben Chlorothricin Ansatrienin B Povidone iodine A10994 XAV 939 Cefmenoxime hydrochloride Acetohydroxamic acid Sodium sulfadiazine Tedizolid Phosphate Triclosan L-Ornithine Dapson Butylparaben Aloperine Amikacin disulfate Aminothiazole Amoxicillin Sodium Ampicillin Trihydrate Azithromycin Dihydrate Azlocillin sodium salt Capreomycin Sulfate Carsalam Cefazolin Sodium Ceftriaxone Sodium Trihydrate Climbazole Clindamycin Clindamycin Phosphate Clioquinol Clopidol Closantel Closantel Sodium Cloxiquine Colistin Sulfate Cyromazine MK-4101 A16229 RU-SKI 43 A16349 HPI-4 Nature communications, 2016, 7, XAV 939 purchased from Adooq XAV 939 is a TNKS inhibitor (IC50 values are and μm for TNKS1 and TNKS2 respectively). Available package size: 10,25,50,100mg A11039 ICG-001 A12362 KY02111 A12707 IWP-2 A12737 A12816 β-catenin A11039 IWR-1-endo LGK-974 ICG-001 Oncogene, 2015, 34(38), LGK-974 purchased from Adooq LGK974 is a highly potent, selective and orally bioavailable Porcupine inhibitor (Wnt signaling antagonist) with an IC50 <1 nm in the Wnt signaling reporter assay and Porcupine binding assay. Available package size: 5,10,25,50mg A12951 Wnt-C59 A13192 IWP-3 A13978 IWP-L6 A15229 Salinomycin sodium salt A15840 ETC-159 A15851 BML-284 (Wnt agonist 1) A15856 PRI-724 A16064 IQ-1 A16094 WAY A16198 Cardiogenol C HCl A16216 CCT A16217 Hexachlorophene A16219 JW74 A16353 KYA1797K Scientific Reports volume 5, 9979 ICG-001 purchased from Adooq ICG-001 is a specific inhibitor of Wnt/β-catenin signaling pathway that inhibits β-catenin/cyclic AMP response element-binding (CREB) protein transcription (IC50=3 microm). Available package size: 5,10,25,100mg A12737 IWR-1-endo A13795 FH535 A13986 WAY A14381 BC2059 A15773 Cardiogenol C hydrochloride A15856 PRI-724 A16064 IQ-1 A16198 Cardiogenol C HCl A16217 Hexachlorophene A16218 icrt 14 A16353 KYA1797K Casein Kinase A10344 Ellagic acid A11781 PF A13574 LH 846 A13584 A-3 Hydrochloride A13949 D4476 A13977 TMCB The higher the number of " " is, the more potent the inhibitor or activator is."" refers to compounds which do Inhibitor Name CK1 CK2 Other Targets CK1δ IC50:250 nm; LH 846 CK1ε IC50: 1.3 μm; CK1α IC50: 2.5 μm D 4476 IC50: 300 nm ALK5 DMAT IC50: 0.13 um IC 261 IC50: 16 μm PF CK1ε IC50: 7.7 nm; CK1δ IC50: 14 nm Silmitasertib IC50: 1 nm SR-3029 IC50: 90 nm TA-01 CK1ε IC50: 6.4 nm; CK1δ IC50: 6.8 nm p38α TBB IC50: 0.9 μm (rat liver)/ IC50: 0.9 μm (human recombinant) TMCB IC50: 0.50 μm ERK8 TTP-22 IC50: 0.1 μm JNK3, ROCK1, and MET A11060 Smoothened A11480 A12774 A12775 A13204 A13627 GSK-3 CX-4945 (Silmitasertib) Nat Commun. 2016; 7: CX-4945 (Silmitasertib) purchased from Adooq CX-4945 is a potent and selective orally bioavailable small molecule inhibitor of CK2 that inhibits human umbilical vein endothelial cell migration, tube formation, and blocks CK2-dependent hypoxiainduced factor 1 alpha (HIF-1α) transcription in cancer cells. Available package size: 2,5,10,50mg A14101 TTP-22 A15069 DMAT A15257 TBB A15764 IC 261 A16234 CX-4945 sodium salt A16235 SR-3029 A16236 TA-01 Purmorphamine LDE225 Diphosphate PF BMS (XL-139) SAG SAG is a chlorobenzothiophene-containing compound which acts as a SMO agonist (EC50 = 3 nm) but inhibits hedgehog signaling at high concentrations (>1 um). Available package size: 2,5,10mg A13881 PF A16221 Jervine Detailed product information is on Page 19.

46 83 Stem Cells / Wnt Membrane Transporters/ 84 Ion Channels Hippo A12658 ATPase A10086 A10213 A10669 A10672 CFTR A10675 A10758 A10985 A10986 Verteporfin γ-secretase Detailed product information is on Page 72. Membrane Transporters/Ion Channels Artemisinin Ciclopirox Oligomycin A Omeprazole Oridonin (Isodonol) PTC124 (Ataluren) VX-770 (Ivacaftor) VX-809 (Lumacaftor) Sci Rep Jan 10;8(1):271. Verteporfin purchased from Adooq Verteporfin is a small molecule that inhibits TEAD YAP association and YAP-induced liver overgrowth. It is also a potent secondgeneration photosensitizing agent derived from porphyrin. Available package size: 5,10,25,50mg A10854 Sodium orthovanadate A11156 Brefeldin A A11408 PF A11696 Pantoprazole (Protonix) A11961 Bafilomycin A1 A12022 Bufalin A12023 Resibufogenin A12024 Bufotalin A12032 Cinobufagin A12755 Ouabain A13041 PST-2744 (Istaroxime) A13283 Rostafuroxin (PST-2238) A13647 (-)-Blebbistcitin A13912 Melittin A14000 Oligomycin A14002 Cyclopiazonic Acid A14007 Thapsigargin A14308 BTB06584 A14875 Glucagon (19-29), human Omeprazole is a cell-permeable, selective proton pump inhibitor. Available package size: 50,100,250,500mg Sci Rep Jul 17;5: VX-809 (Lumacaftor) purchased from Adooq Available package size: 5,10,25,50mg A16228 Calcium Channels A10068 A10069 A10215 A10219 A10309 A10311 A10487 A10553 A10554 A10643 A10645 A10921 A11140 A11206 XMU-MP-1 A12519 VX-661 A12897 CFTRinh-172 A13000 PPQ-102 A13511 IOWH032 A13723 CFTR-Inhibitor-II A15843 KM Amlodipine Amlodipine besylate (Norvasc) Cilnidipine AMG-073 HCl (Cinacalcet HCl) Diethylstilbestrol Diltiazem HCl Isradipine Manidipine (Manyper) Manidipine 2HCl Nifedipine Nimodipine Tetrandrine (Fanchinine) NPS-2143 (SB ) CK (Omecamtiv mecarbil) Journal of Biological Chemistry, 2017, 292(9): CK (Omecamtiv mecarbil) purchased from Adooq CK is a selective cardiac specific myosin activator. Available package size: 5,10,50,100mg A11219 Azelnidipine A11314 AMG 073 (Cinacalcet) A11405 Astragaloside A A11729 Lacidipine A11730 Benidipine hydrochloride A11731 Nilvadipine (ARC029) A11746 Clevidipine A12405 NS6180 A12482 Mibefradil dihydrochloride A12684 Pinaverium Bromide A13402 Atagabalin A13928 Dantrolene A13989 BAPTA tetrapotassium A14023 BAPTA/AM A14794 Berbamine A14935 (S)-Amlodipine A15188 NNC A15192 NP A15875 Bay K 8644 A16146 Dantrolene sodium A16346 YM A16444 Chlorocresol A16454 Cinepazide maleate A16455 Cinnarizine Sodium Channels A10064 Amiloride HCl A10168 Bupivacaine HCl A10179 Carbamazepine A10510 Lacosamide A10530 Lidocaine (Alphacaine) A10721 Phenytoin (Lepitoin) A10722 Phenytoin sodium (Dilantin) A10795 Riluzole (Rilutek) A11102 PF A11234 A A11602 Vinpocetine A11712 Orphenadrine citrate A11715 Proparacaine HCl A11728 Amiloride hydrochloride dihydrate A11750 Ibutilide fumarate A11873 Lamotrigine A13760 QX 314 chloride A13773 A13898 A13900 A13943 A14011 ICA Encainide HCl Disopyramide Oxcarbazepine Tenapanor QX 314 chloride is a membrane impermeable quaternary derivative of lidocaine, a voltageactivated Na+ channel blocker. Available package size: 50,100,250mg Molecular and Cellular Biochemistry, 2017, 427: 201. Tenapanor purchased from Adooq Tenapanor acts as an inhibitor of the sodium-proton exchanger NHE3. This antiporter protein is found in the kidney and intestines, and normally acts to regulate the levels of sodium absorbed and secreted by the body. Available package size: 2,5mg A14139 ENIPORIDE A14240 Procainamide HCl A14242 Digoxin A14260 Chloroprocaine HCl A14361 GS967 A14560 Benzocaine A15088 Flecainide acetate A15228 S0859 A15243 Sodium Channel inhibitor 1 A15275 Vernakalant HCl A15422 beta-pompilidotoxin A15979 Levobupivacaine A16130 Benzocaine hydrochloride A16131 Procaine A16362 Pilsicainide HCl A16365 PF A16398 Ambroxol HCl Potassium Channels A10430 A10433 A10455 A10593 A10629 A10641 A10783 A11239 A11521 A11712 A11884 A11922 Glimepiride Glyburide Hydralazine hydrochloride Minoxidil (U-10858) Nateglinide (Starlix) Nicorandil Repaglinide TAK-438 (vonoprazan) PAP-1 (5-(4-Phenoxybutoxy)psoralen) Orphenadrine citrate Mitiglinide calcium Retigabine (Ezogabine) J Neurosci Feb 4; 35(5): Retigabine (Ezogabine) purchased from Adooq Retigabine is an anticonvulsant used as a treatment for partial epilepsies. Available package size: 25,50,100,250mg A11934 NS 309 A12783 TRAM-34 Cell Death & Disease volume 4, page e773 (2013) TRAM-34 purchased from Adooq TRAM-34 is a highly selective blocker of intermediate conductance Ca2+-activated K+ channels (KCa3.1) (Kd = 20 nm). Exhibits fold selectivity over KV, BKCa, KCa2, Na+, CRAC and Clchannels. Suppresses the reactivation of lymphocytes by mitogenic stimuli. Available package size: 10,25,50,100mg A12857 E-4031 dihydrochloride A13944 GW X A HETE A15222 Retigabine dihydrochloride A15275 Vernakalant HCl