Adooq Bioscience. Kinase Inhibitors Catalog Innovation through Bioscience.

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1 Adooq Bioscience Innovation through Bioscience Kinase Inhibitors Catalog Adooq Bioscience LLC Barranca Parkway, Suite 250 Irvine, CA 92604, USA Phone: Fax:

2 I About Us Distributors II Who We Are Adooq Bioscience is one of the world leading suppliers of high-performance lifescience reagents and reference compounds for the research fields. Now, Adooq has more than 4200 products with validated biological and pharmacological activities, and an unique collection of over 2000 inhibitors on HDAC, PI3K, Apoptosis and more signaling pathways in stock. Global Scope About Us Adooq has more than 25 distributors in 30 different countries all over the world. Our worldwide marketing network supports first-class service on five continents. Australia Canada China France Hungary Worldwide Distributors Sapphire Bioscience Pty. Ltd. Tel: Fax: Cedarlane Tel: +1(289) Fax: +1(289) Guangzhou Whiga Technology ltd. Tel: Fax: CliniSciences Tel: Fax: Bio-Science Ltd. bio-sci@bio-science.hu Tel: (06-1) Fax: (06-1) Austria China China Germany India Hölzel Diagnostika Handels GmbH info@hoelzel.de Tel: +49(0) Fax: +49(0) Shenzhen Minn Bolin Bio-Tech Co., Ltd. peacerli@mbolin-lktlabs.com Tel: Fax: ADVANCED TECH. & IND. CO., LTD. mandy@advtechind.com Tel: Fax: Hölzel Diagnostika Handels GmbH info@hoelzel.de Tel: +49(0) Fax: +49(0) Biogenuix Medsystems Pvt Ltd contact@biogenuix.com Tel: Fax: Technology and Quality Indonesia PT Sciencewerke. enquiry@sciencewerke.com Tel: Fax: Ireland Bioquote Limited sales@bioquote.com Tel: Fax: Adooq focuses on technologies that improve our ability to find, develop and produce life-science reagents. The safety and effectiveness of all Adooq products has been demonstrated through preclinical and clinical research. Israel ENCO Scientific Services info@enco.co.il Tel: Fax: Italy CliniSciences italia@clinisciences.com Tel: Fax: Quick Delivery Japan FUNAKOSHI CO., LTD. info@funakoshi.co.jp Tel: Fax: Lebanon DPC/LEBANON SARL info@dpcleb.com Tel: Fax: For U.S. based customers, Adooq guarantees that orders placed by 3:30 p.m. (U.S. Pacific Time) will arrive the next day 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. Malaysia New Zealand Sciencewerke Sdn Bhd enquiry@sciencewerke.com Tel: Fax: Sapphire Bioscience (NZ) Ltd. sales@sapphirebioscience.com Tel: Fax: Morocco Singapore HexaBiogen maroc@hexabiogen.com Tel: Fax: Sciencewerke Pte Ltd. enquiry@sciencewerke.com Tel: Fax: Our Mission South Korea Bioclone Corp. bioclone@bioclone.co.kr Tel: Fax: South Korea LeehyoBioscience Co., Ltd support@leehyobio.com Tel: Fax: ~3 Adooq recognizes that the world needs the life-science reagents, especially some inhabitiors for the cancer research, in every potential form. That s why Adooq s employees work to responsibly develop the affordable, reliable lifescience reagents the world needs. You are welcomed to join or work with us creating innovations that matter to people! Spain Taiwan CliniSciences espana@clinisciences.com Tel: Fax: ASIA BIOSCIENCE CO.,LTD. jimmy@abscience.com.tw Tel: Fax: Switzerland United Kingdom Hölzel Diagnostika Handels GmbH info@hoelzel.de Tel: +49(0) Fax: +49(0) Bioquote Limited sales@bioquote.com Tel: Fax:

3 III Contents Contents IV Apoptosis...1 Bcl-2 Family 1 Caspase 1 p53 1 TNF-α 1 IAP 1 RasGAP (Ras- P21) 2 PERK 2 Angiogenesis...2 EGFR / HER2 2 MDM2 2 Apoptosis Inducers 2 FGFR 3 PDGFR 3 VEGFR 3 Vascular Disrupting Agent (VDA) 4 HIF 5 MAPK...5 MEK/ERK 5 5-alpha-reductase 5 Antiangiogenics 5 p38-mapk 6 JNK/c-Jun 6 Raf 6 Cell Cycle...7 Checkpoint Kinase 7 cyclin-dependent kinases (CDKs) 8 Checkpoint Control Kinases 9 Aurora Kinase 9 PARP 9 Polo-like kinases (PLKs) 10 Rho-Kinase (ROCKs) 10 Topoisomerase 11 Microtubules 11 Synthases / Synthetases 12 RNA/DNA Polymerase 12 Telomerase 12 Ligases 12 Reverse Transcriptase 12 Cell Metabolism...13 Cytochrome P Mitosis 13 β-amyloid 14 Phosphodiesterases (PDEs) 14 Hydroxylases 14 Dihydrofolate reductase (DHFR) 15 Dehydrogenases 15 Cyclooxygenase (COX) 15 Antimetabolite 16 Histone Deacetylase (HDAC) 16 Sir2-like Family Deacetylases (sirtuins) 17 Monoamine Oxidase (MAO) 17 Factor Xa 17 Kinesin Spindle Protein 18 DNA, RNA and Protein Synthesis 18 CYP17 18 Phospholipases 19 Lipid Metabolism 19 FAAH 19 CETP 19 DNA Methyltransferases 19 HMG-CoA Reductase 19 Neuronal Metabolism 19 IDO 19 Contents PI3K / Akt / mtor...20 Akt 20 Ferroptosis 20 PI3-Kinase (PI3K) 20 mtor 22 PDK1 23 Receptor Tyrosine Kinases...23 EGFR/HER2 23 DNA-dependent protein kinase (DNA-PK) 23 Ribosomal S6 protein kinases (RSK) 23 FGFR 24 PDGFR 24 VEGFR 24 Type 1 insulin-like growth factor receptor (IGF-1R) 24 FLT3 (FMS-like tyrosine kinase 3) 25 c-met 25 ALK 25 BCR-ABL 26 FAK 26 SRC 26 c-kit 27 Spleen tyrosine kinase (Syk) 27 Tie-2 27 Bone Morphogenetic Proteins (BMP) 28 Bruton's tyrosine kinase 28 NF-kB/IkB...28 NF-kB 28 Axl 28 Tyrosine kinase 28 Trk Receptors 28 Cytokines 29 IKK 29 JAK / Stat...29 JAK 29 Stat 29 Pim Kinase 29 TGF-β / Smad...30 TGF-β / Smad Inhibitors 30 Protein Kinase C (PKC) 30 Proteases...30 Caspase 30 Protein Kinase A 30 Protein kinase D (PKD) 30 Proteasome 30 HCV Protease 31 HIV Protease 32 Heat Shock Proteins (HSP) 32 Aminopeptidase 33 Integrase 33 Dipeptidyl Peptidase IV (DPP-4) 33 Thrombin 33 Angiotensin-Converting Enzyme (ACE) 33 Matrix Metalloprotease 33 Other Proteases 33 MMP 34 Epigenetics...34 Bromodomain 34 Stem Cells...34 Stem Cell Proliferation 34 Cathepsin 34 Histone demethylases 34 Stem Cell Differentiation 34 GSK-3 / Wnt / Hedgehog...35 γ-secretase 35 Hedgehog 35 Wnt 35 β-catenin 36 GSK-3 36 Smoothened 36 Transporters...37 ATPase 37 Multidrug Transporters 37 Sodium-dependent Glucose Cotransporter (SGLT) 37 Monocarboxylate transporters (MCT) 37 Neurotransmitter Transporters 38 AMPA receptor 38 Ion Channels...38 Calcium Channels 38 P-gp 38 CRM1 38 Ligand-gated Ion Channels 38 Sodium Channels 39 Potassium Channels 39 Chloride Channels 39 Cystic Fibrosis Transmembrane Regulator (CFTR) 39 Transient Receptor Potential Channels 40 AMPK / Insulin Receptor...40 AMPK 40 ATM / ATR...40 ATM 40 NMDA Receptors 40 ATR 40 7-TM Receptors HT Receptors 41 Adrenergic Receptors 41 Acetylcholine Muscarinic Receptors 42 Histamine Receptors 42 Dopamine Receptors 42 Opioid Receptors 42 GABA Receptors 42 Purinergic (P2Y) Receptors 42 Metabotropic glutamate receptors (mglur) 43 Angiotensin Receptors 43 Melatonin Receptors 43 Peptide Receptors 43 Smoothened Receptors 43 Chemokine Receptors (CCR5) 43 G Protein 43 Platelet-Activating Factor (PAF) Receptors 43 Endothelin Receptors 43 P2X Receptor 43 LPA Receptor 43 Prostanoid Receptors 43 Adenosine Receptors 44 Cannabinoid Receptors 44 Neurotensin Receptors 44 Endocrinology / Hormones...44 Pregnane X Receptors 44 Estrogen Receptors 44 Leukotriene receptor 44 Orexin Receptors 44 Somatostatin Receptors 44 NK1 Receptors 44 Protease-Activated Receptors (PAR) 44 Progesterone Receptors 44 Renin-angiotensin-aldosterone system (RAAS) 45 Androgen Receptors 45 PPAR 45 Liver X receptors (LXRs) 45 Aromatase 46 Retinoic Acid Receptors 46 Glucocorticoid receptors 46 Transferases...46 Glucocorticoid receptors 46 Vitamin D Receptors 46 GnRH receptor 46 GPR 46 Phosphorylases 46 Methyltransferases 47 Protein Prenyltransferases 47 FPTase 47 Histone Methyltransferase 47 Histone Acetyltransferases 47 DNA Methyltransferases 47 Ubiquitin...48 activating enzyme E1 48 E3 ubiquitin ligase 48 DUB 48 Others...48 Other inhibitors 48 p97 48 Carbonic Anhydrase 54 Cholinesterase 54 Casein Kinase 2 54 Soluble guanylyl cyclase (sgc) 54 Reagents 54 Integrin Receptors 54 Toll-like Receptors 54 Beta-secretase (BACE) 54 LRRK2 54 MELK 54 β-lactamase 55 Gluconeogenesis 55 Cholinesterases 55 Aldose Reductase 55 Nitric Oxide Signaling 55 Adenylyl Cyclase 55 IDH1 55 LSD1 inhibitor 55 Casein Kinase 1 55 Lipoxygenase 55 Sigma-1 receptor 55

4 1 Apoptosis Apoptosis 2 Bcl-2 Family A10022 ABT-263 (Navitoclax) A10255 ABT-737 Apoptosis VX-765 is a novel Caspase-1 inhibitor,which is an enzyme that controls the generation of two cytokines, IL-1b and IL-18. A11090 PAC-1 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 A11163 A11928 A12738 AT-406 LCL-161 Birinapant (TL32711) RasGAP (Ras- P21) MDM2 A10657 A11179 A11501 A11502 A13582 Nutlin-3 NSC (XI-006) Nutlin 3a Nutlin 3b MDM2 Inhibitor A11944 Apoptosis Activator 2 A12373 A13070 Z-VAD-FMK LY (Tasisulam) A10935 A11225 A11930 Tipifarnib (Zarnestra) Pluripotin (SC-1) PF p53 A10491 JNJ MDM2 antagonist Nutlin-3 is a potent inducer of apoptosis. *Available package size: 5,25,50,100mg 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). A10665 A10955 A11448 A12500 A12743 A12823 Obatoclax mesylate (GX15-070) TW-37 HA14-1 ABT-199 BM-1074 Sabutoclax A12907 BAM 7 A13578 AT101 JNJ is one of p53-activating agents and synergizes with AraC or doxorubicin to induce p53-mediated apoptosis and may provide a novel therapeutic approach for the treatment of acute leukemias. A11931 RITA (NSC ) A11943 A12305 A12449 A12450 A12451 Tenovin-1 Tenovin-6 Pifithrin-u Pifithrin-beta Pifithrin-alpha A12930 NSC A13581 A13727 TNF-α PRIMA-1 Tenovin-3 PF is a small-molecule p21-activated kinase inhibitor inhibiting oncogenic signaling and tumor growth. A13750 PERK A12792 A13577 A13816 GSK GSK EGFR / HER2 A10043 A10047 Hypothemycin ISRIB (trans-isomer) AEE788 AG-490 Apoptosis Inducers A10582 A11279 A11635 A11988 Methylprednisolone FK866 Cyclophosphamide monohydrate Gambogic acid Angiogenesis AT101, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl- 2, Bcl-xL and Mcl-1 with Ki of 0.32 μm, 0.48 μm and 0.18 μm; does not inhibit BIR3 domain and BID. Caspase A10984 VX-765 A10522 Lenalidomide (CC-5013) A10743 Pomalidomide (CC-4047) A11957 Bay A11973 Necrostatin-1 A12748 QNZ IAP A11002 YM155 AG-490 is a selective inhibitor of EGF receptor tyrosine kinase (IC50 values are 2 and 13.5 μm for EGFR and ErbB2 respectively). *Available package size: 10,50,100,200mg A10053 Tyrphostin AG 879 A10062 A10116 A10141 A10210 A10211 A10242 AST-6 AZD8931 BIBW2992 (Afatinib) Chrysophanic acid (Chrysophanol) Canertinib (CI-1033) CP BIBW2992 (Afatinib) is tyrosine kinase inhibitor (TKI) that irreversibly inhibits human epidermal growth factor receptor 2 (Her2) and epidermal growth factor receptor (EGFR) kinases. *Available package size: 5,10,25,100mg A10362 A10422 A10514 Erlotinib Hydrochloride Gefitinib (Iressa) Lapatinib Ditosylate A10612 Mubritinib (TAK 165) A10638 A10678 A10702 A10706 Neratinib (HKI-272) OSI-420 PD (HCl salt) Pelitinib (EKB-569)

5 3 Angiogenesis Angiogenesis 4 A10990 A10991 A10992 A11022 A11027 WZ3146 WZ4002 WZ8040 AG-1478 (Tyrphostin AG-1478) Arry-380 A12650 PKC 412 A10049 A10101 A10103 A10137 Albendazole Tivozanib (AV-951) Axitinib Bibf1120 (Vargatef) TSU-68 (SU-6668) is an inhibitor of RTKs involved in VEGF, bfgf and PDGF signaling, which inhibits endothelial cell proliferation. A10963 A10967 A10996 Vandetanib (ZD6474) Vatalanib (PTK787) 2HCl Base XL184 free base (Cabozantinib) ARRY-380 is an ErbB-2 inhibitor that selectively binds to and inhibits the phosphorylation of ErbB-2, resulting in growth inhibition and death of ErbB-2-expressing tumor cells. A11028 A11051 A11057 A11155 A11158 A11209 A11236 A11263 AV-412 PF XL647 AST-1306 ARRY BMS (AC480) TAK-285 TAK-285 is an investigational HER2/EGFR inhibitor that penetrates the CNS in Rats with an Intact Blood Brain Barrier (BBB). BMS A11334 BIBX 1382 PKC 412 is a broad spectrum protein kinase inhibitor. Inhibits conventional PKC isoforms (α, β, γ), PDFRβ, VEGFR2, Syk, PKCη, Flk- 1, Flt3, Cdk1/B, PKA, c-kit, c-fgr, c-src, VEGFR1 and EGFR. Displays potent antitumor activity. *Available package size: 5,10,25mg A12867 A12868 FGFR A10703 A11075 A11159 PD AZD4547 BGJ398 (NVP-BGJ398) A11244 LY PDGFR A10504 KRN 633 A10880 Sunitinib Malate A10903 Telatinib (BAY ) A11052 A11350 CGP ARRY-543 A13588 Tyrphostin AG 183 A13681 A13718 A13755 A13825 AZD-9291 Icotinib Hydrochloride CNX-2006 Icotinib Crenolanib (CP ) CP A11581 Toceranib (PHA , SU 11654) BIBF1120 (Vargatef) is a novel triple angiokinase inhibitor that inhibits three growth factor receptors simultaneously: VEGFR, PDGF and FGFR. A10162 A10185 A10204 A10248 A10254 Brivanib alaninate (BMS ) Cediranib (AZD2171) Chloroxine CYC116 Brivanib (BMS ) Brivanib (BMS ) is a VEGFR -2 inhibitor with an IC50 of 25 nm and Ki of 26 nm. *Available package size: 5,10,50,200mg A10259 A10340 Imatinib (Gleevec) E7080 (Lenvatinib) XL184 free base (Cabozantinib) is a small molecule designed to inhibit multiple receptor tyrosine kinases, specifically MET and VEGFR2. A11396 A11496 A11557 A11772 A11954 A11955 A12027 A12437 SU 5416 is an inhibitor of vascular endothelial growth factor receptor (VEGFR) that also inhibits other tyrosine kinases KIT, MET, FLT3 and RET. A13234 A13377 A13465 A13966 E-7050 (Golvatinib) Motesanib (AMG706) SU14813 CP ZM hydrochloride ZM hydrochloride (-)-Catechin gallate SU 5416 (Semaxinib) SKLB1002 SAR SKLB610 TPT-260 (Dihydrochloride) E7080 is a multi-kinase inhibitor that inhibits both VEGFR2 and VEGFR3 kinases. BIBX 1382 is a cell-permeable pyrimido-pyrimidine compound that acts as a potent, reversible, ATP-competitive, and highly selective inhibitor of EGFR. *Available package size: 5,10,25mg A11407 A11558 Apatinib (YN968D1) SU-5402 Toceranib is a kinase inhibitor with both antitumor and antiangiogenic activity through inhibition of KIT, vascular endothelial growth factor receptor 2, and PDGFRβ. A11753 A11978 VEGFR MK-2461 Delphinidin chloride A10495 A10502 A10608 A10699 A10893 A10953 Kaempferol Ki8751 Motesanib Diphosphate (AMG-706) Pazopanib Hydrochloride (GW786034) Taxifolin TSU-68 (SU6668) TPT-260 is a thiophene thiourea derivative. Vascular Disrupting Agent (VDA) A10324 DMXAA (ASA404) A11752 A11948 A11949 A12448 Lapatinib (free base) AP26113 AG-17 Butein A10025 Linifanib (ABT-869) Linifanib (ABT-869) is a structurally novel, potent inhibitor of RTK, VEGF and PDGF with IC50 of 0.2, 2, 4, and 7 nm for human endothelial cells, PDGFR-β, KDR, and CSF-1R, respectively.

6 5 Angiogenesis MAPK 6 DMXAA (ASA404) is a tumor-vascular disrupting agent (tumor-vda) that attacks the blood supply of a cancerous tumor to cause tumor regression. *Available package size: 5,25,50,100mg A10654 HIF A10012 A11237 NPI-2358 (Plinabulin) 2-Methoxyestradiol FG alpha-reductase A10037 A10188 A10338 A10387 A10631 Aciclovir (Acyclovir) Cefditoren pivoxil Dutasteride (Avodart) Finasteride Antiangiogenics A12601 Nefiracetam (Translon) Combretastatin A4 A11441 A11493 A11794 A12002 A12505 A12824 GDC-0973 MEK162 (ARRY ) VRT Arctigenin TCS ERK 11e (VX-11e) SCH SB is a specific inhibitor of p38α and p38β which suppresses downstream activation of MAPKAP kinase-2 and heat shock protein 27. *Available package size: 25,50,100,200mg A10976 Vinorelbine (Navelbine) A10982 A10983 A11078 VX-702 VX-745 PH A11221 PD A11321 Skepinone-L A11562 SB A11582 TAK-715 A12021 Asiaticoside SCH is a novel, specific inhibitor of ERK-1/2 with IC50 of 4 nm and 1 nm, respectively. A12408 A12770 ML-3043 Talmapimod (SCIO-469) FG-4592 is a novel hypoxia inducible factor prolyl hydroxylase inhibitor, in CKD anemia. A11924 IOX 2 A12883 A12921 FM19G11 HIF-C2 A12978 BAY Combretastatin A4 is an antitumor, anti-angiogenic and antimetastatic agent, in vitro and in vivo. Inhibits tubulin polymerization. A12866 Refametinib (RDEA-119, BAY ) A13135 A13272 A13420 A14019 Kobe0065 RO GDC0994 RO Talmapimod (SCIO-469) is a selective, ATP-competitive p38 inhibitor (IC50 = 9 nm for p38α in vitro). MEK/ERK A10089 AS A10115 AZD8330 A10150 BIX02188 A10151 BIX MAPK A10257 A10453 A10704 A10705 AZD6244 (Selumetinib) Honokiol PD PD98059 RO , also known as CH , is a protein kinase inhibitor specific for the Raf and MEK mitogen-activated protein kinases (MAPKs) with potential anti-neoplastic activity. *Available package size: 5,10,25mg p38-mapk A10092 A10148 Asiatic acid Doramapimod (BIRB-796) JNK/c-Jun A10860 SP A11296 AS (Bentamapimod) A11352 CC-401 A11969 TCS JNK 5a PD98059 is an equipotent antagonist of the aryl hydrocarbon receptor and inhibitor of mitogen-activated protein kinase kinase. *Available package size: 10,50,100,200mg TCS JNK 5a is a highly selective inhibitor of JNK2 and JNK3 (pic50 values are 6.7, 6.5, <5.0 and <4.8 for JNK3, JNK2, JNK1 and p38?? respectively). *Available package size: 10,25,50mg A12749 JNK-IN-8 BIX02188 is a potent and selective inhibitor of MEK5. A10212 PD (CI-1040) A10256 PD A10957 A11029 A11040 A11247 U0126-EtOH GSK (JTP-74057, Trametinib) TAK-733 RO Doramapimod (BIRB 796) is a small molecule inhibitor of p38 MAPK,which plays a critical role in regulating the production of proinflammatory cytokines. A10545 LY A10823 SB A10824 SB Raf A10001 A10002 A10420 A10661 A10739 Sorafenib (Nexavar) PLX-4720 GDC-0879 NVP-BHG712 PLX4032 (Vemurafenib) PD is MEK inhibitor and non-competitive with ATP, Kiapp of 1 nm against activated MEK1 and MEK2. *Available package size: 5,10,25,100mg RO is a potent and highly selective non-atp-competitive MEK1/2 inhibitor.

7 7 MAPK Cell Cycle 8 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) RAF265 (CHIR-265) is an oral, highly selective RAF and VEGFR kinase inhibitor, which is to control or normalize VEGFR-2 along with the inhibition of B-raf and c-raf mutation to prevent cancers. A11436 GW 5074 A12578 A12739 A12891 Kobe2602 PF Diazepinomicin A13226 LGX 818 LGX818 is an orally available Raf kinase inhibitor with potential antineoplastic activity. *Available package size: 1,5,10,25mg SCH is an agent targeting cell cycle checkpoint kinase 1 (Chk1) with potential radiosensitization and chemosensitization activities. A13403 A13575 cyclin-dependent kinases (CDKs) A10093 ZCL-278 BML-277 AT7519 SNS-032 (BMS ) is a highly selective and potent inhibitor of cyclin-dependent kinases (Cdks) 2, 7, and 9, with in vitro growth inhibitory effects and ability to induce apoptosis in malignant B cells. A11045 A11047 A11105 Flavopiridol HCl PHA (Milciclib) AZD5438 A11129 Dinaciclib (SCH ) A11154 A11164 A11190 A11220 BMS PHA R547 Kenpaullone A10774 A10829 A11063 Raf265 derivative SB AZ628 A11077 ZM A11240 A11333 A11381 MLN2480 (BIIB-024) BRAF inhibitor Dabrafenib (GSK A) A13323 TAK-632 A13525 L 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 A10163 A10390 BS-181 HCl Flavopiridol (Alvocidib) Kenpaullone is a potent inhibitor of CDK1/cyclin B (IC₅₀ = 400 nm), CDK2/cyclin A (IC₅₀ = 680nM), CDK5 (IC₅₀ = 850nM) and with much less effect other kinases. *Available package size: 10,50,100mg A11313 A11347 A12352 AT7519 HCl CGP60474 Purvalanol B A12438 NU 6102 A12742 BAY A12989 LY Dabrafenib is a potent and selective inhibitor of B-RAF protein kinase carrying V600E mutation, currently in clinical trial. *Available package size: 5,25,50,100mg A13454 SB1317 (TG-02) A13547 P Cell Cycle Flavopiridol (Alvocidib) is a cyclin-dependent kinase inhibitor under clinical development for the treatment of chronic lymphocytic leukemia. Checkpoint Kinase A10113 AZD7762 A10599 MK-1775 A10494 A10701 JNJ PD HCl P276-00, a novel cyclin-dependent inhibitor induces G1-G2 arrest, shows antitumor activity on cisplatin-resistant cells and significant in vivo efficacy in tumor models. *Available package size: 5,10,25mg A13549 LEE011 MK-1775 is a potent and selective Wee1 kinase inhibitor in vitro and in vivo. A11036 A11046 LY (IC-83) CHIR-124 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 A11108 A11167 CCT A11520 PF A12703 SCH (MK-8776) SCH PD HCl is an orally available pyrido-pyrimidine-derived cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity. A10716 PHA A10806 A10850 Roscovitine (Seliciclib) SNS-032 (BMS ) A13677 BMS (XL-413) BMS , also known as XL-413, is an orally bioavailable cell division cycle 7 homolog (CDC7) kinase inhibitor with potential antineoplastic activity. A13721 TG003

8 9 Cell Cycle Cell Cycle 10 Checkpoint Control Kinases A11036 A11108 LY (IC-83) CCT 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) A10135 A10442 A10452 A10673 BI6727 (Volasertib) GSK HMN-214 ON Aurora Kinase A10004 MLN8237 (Alisertib) VX-680 is a potent and selective small-molecule inhibitor of the Aurora kinases. *Available package size: 25,50,100,250mg A11009 ZM A10164 BSI-201 (Iniparib) A11066 AMG 900 A11067 A11081 A11168 A11171 TAK-901 CCT GSK PF BSI-201 is a potent inhibitor of PARP-1 and has been shown to cross the blood-brain barrier. *Available package size: 10,50,100,200mg ON is selectively cytotoxic for chronic lymphocytic leukemia cells through a dual mechanism of action involving PI3K/AKT inhibition and induction of oxidative stress. MLN8237 (Alisertib) is a selective Aurora kinase A inhibitor with a median IC50 of 61 nm. *Available package size: 5,10,50,200mg A11410 MK-5108 (VX-689) A10475 A10909 A11026 INO-1001 Tenofovir Disoproxil Fumarate MK-4827 A11146 TAK-960 A10095 AT9283 A10100 A10109 Aurora A Inhibitor I AZD1152-HQPA (Barasertib) MK-5108, also known as VX-689, is a competitive inhibitor of the ATP-binding site of aurora A kinase. A13250 A13396 Reversine MK-8745 MK-4827 is a novel potent, orally bioavailable PARP-1 and PARP-2 inhibitor. *Available package size: 5,10mg A11243 BMN673 TAK-960 is a novel, orally available, selective inhibitor of polo-like kinase 1, shows broad-spectrum preclinical antitumor activity. A11438 GW843682X A12429 MLN 0905 A13245 RO3280 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: 5,10,50,200mg A10184 CCT A10248 A10448 CYC116 Hesperadin PARP A10019 A A displayed high potency against the poly(adp-ribose) polymerase-1 (PARP-1) enzyme with a K(i) of 1 nm and an EC(50) of 1 nm in a whole cell assay. A10026 ABT-888 (Veliparib) BMN-673 is an orally bioavailable inhibitor of the nuclear enzyme poly(adp-ribose) polymerase (PARP) with potential antineoplastic activity. A12393 A12665 AZD-2461 A12750 UPF 1069 A13731 JW 55 PJ 34 hydrochloride Rho-Kinase (ROCKs) A10381 Fasudil HCl (HA-1077) Fasudil HCl is a cyclic nucleotide-dependent protein kinase inhibitor and Rho-associated kinase inhibitor (IC50 = 10.7 μm). *Available package size: 250,500mg A10441 A10928 GSK429286A Thiazovivin Polo-like kinases (PLKs) Hesperadin is a human Aurora B inhibitor with an IC50 of 40 nm for the prevention of the phosphorylation of substrate. A10601 A10714 A10715 A10851 A10981 MLN8054 PHA Danusertib (PHA ) SNS-314 VX-680 (MK-0457, Tozasertib) ABT-888(Veliparib) is a potential anti-cancer drug acting as a PARP inhibitor. *Available package size: 10,50,100,200mg A10045 AG (Rucaparib) A10134 BI 2536 BI 2536 is a selective inhibitor of Plk1, which inhibits Plk1 enzyme activity at low nanomolar concentrations. Thiazovivin is a selective inhibitor of Rho-associated kinase (ROCK). A11001 Y dihydrochloride

9 11 Cell Cycle Cell Cycle 12 Y is a Rho-Associated Coil Kinase (ROCK) inhibitor that increases the cloning efficiency of human embryonic stem cells (hescs). A11610 Y A12348 GSK A12546 NSC A12674 SR 3677 dihydrochloride A10740 A10939 Podophyllotoxin Topotecan HCl (Hycamtin) 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. A10326 A10359 A10360 Docetaxel (Taxotere) Epothilone A Epothilone B (EPO906) A13827 CK-636 Synthases / Synthetases A10050 Alendronate sodium hydrate A10776 Raltitrexed (Tomudex) A12992 HQL-79 A W Dihydrochloride Topotecan HCl (Hycamtin) is a chemotherapeutic agent that is a topoisomerase inhibitor. *Available package size: 50,100,200mg A11231 Exatecan mesylate RNA/DNA Polymerase A10908 A11115 Tenofovir (Viread) Abacavir A11120 Abacavir sulfate SR 3677 dihydrochloride is a potent and selective Rho-kinase inhibitor (IC50 values are 3 and 56 nm for ROCK-II and ROCK-I respectively). A12740 A13067 EHop-016 RKI-1447 RKI-1447 is a potent inhibitor of the Rho-associated ROCK kinases with anti-invasive and antitumor activities in breast cancer. Exatecan mesylate inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA and inhibiting religation of DNA breaks, thereby inhibiting DNA replication and triggering apoptotic cell death. A11861 A11902 Flumequine Pefloxacin mesylate Epothilone B is a macrolide that causes the formation of bundles of intracellular microtubules in non-mitotic cells, induces the formation of hyperstable tubulin polymers, and arrests cell cycling in mitosis. *Available package size: 2,5,10,25mg A10689 Paclitaxel (Taxol) A11590 T-705 (Favipiravir) T-705, a substituted pyrazine compound, has been found to exhibit potent anti-influenza virus activity in vitro and in vivo. A13239 A13274 Telomerase Actinomycin D Delavirdine mesylate A13785 Topoisomerase HA-1077 dihydrochloride A11997 A12011 SN 38 (S)-10-Hydroxycamptothecin A10140 BIBR 1532 A10041 A10071 A10174 A10194 A10345 A10373 A10465 Adriamycin Amonafide (AS1413) Camptothecin Cerubidine Epirubicin Hydrochloride Etoposide (VP-16) Idarubicin HCl SN 38 is the active metabolite of irinotecan (an analog of camptothecin - a topoisomerase I inhibitor). *Available package size: 50,100,250mg A12663 A13059 Amrubicin Beta-Lapachone Paclitaxel (Taxol) is a mitotic inhibitor that stabilizes microtubules and as a result, interferes with the normal breakdown of microtubules during cell division. *Available package size: 10,50,100,200mg A10740 A10973 A10975 A11412 Podophyllotoxin Vincristine sulfate Vinflunine Tartrate Epothilone D 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 A11999 A13093 A13206 Costunolide Betulinic acid Amsacrine GENZ Microtubules Ligases A10024 A10238 ABT-751 Colchicine A10884 TAME Idarubicin is an anthracycline antibiotic that is an anti-leukemia agent with higher DNA binding capacity and greater cytotoxicity than daunorubicin. A10477 A10478 A10479 A10596 A10609 A10735 Irbesartan (Avapro) Irinotecan Irinotecan HCl Trihydrate (Campto) Mitoxantrone Hydrochloride Moxifloxacin HCl Pirarubicin A10264 CYT997 Epothilone D improves microtubule density, axonal integrity, and cognition in a transgenic mouse model of tauopathy. *Available package size: 1,2,5,10mg A11449 A11617 A12591 A12804 A13081 A13219 A13735 Ixabepilone Vinblastine Cevipabulin (TTI-237) Eribulin Mesylate Fosbretabulin disodium (CA4P) Nocodazole CW069 Reverse Transcriptase A10039 A10349 A10639 A10908 Adefovir dipivoxil Emtricitabine Nevirapine (Viramune) Tenofovir (Viread)

10 13 Cell Cycle Cell Metabolism 14 A12587 Dapivirine A13366 Mephenytoin A12667 Lersivirine (UK ) A13367 Methoxyresorufin β-amyloid Tenofovir is in a class of medications called nucleoside reverse transcriptase inhibitors (NRTIs). It works by decreasing the amount of HIV in the blood. A10909 A11115 A11120 A12443 Tenofovir Disoproxil Fumarate Abacavir Abacavir sulfate MK-1439 MK-1439 is a non-nucleoside reverse transcriptase inhibitor. Cytochrome P450 A10020 Abiraterone (CB-7598) Lersivirine (UK-453,061) is a next-generation nonnucleoside reverse transcriptase inhibitor, active against wild-type HIV-1 and several nonnucleoside reverse transcriptase inhibitor-resistant strains. Mitosis A13872 INH1 Cell Metabolism TAK-700 (Orteronel) is an oral, non-steroidal androgen synthesis inhibitor that selectively inhibits the 17,20 lyase enzyme. A10312 A12647 Ro Dimebon dihydrochloride Phosphodiesterases (PDEs) A10216 Cilomilast (SB ) Cilomilast is orally active and acts as a selective Phosphodiesterase-4 inhibitor with antiinflammatory effects that target bronchoconstriction, mucus hypersecretion, and airway remodeling associated with COPD. A10217 Cilostazol A10449 A10464 A10541 A10592 A10733 Hesperetin Icariin Luteolin Milrinone (Primacor) Pimobendan (Vetmedin) Pimobendan (Vetmedin) is a calcium sensitizer with positive inotropic and vasodilator effects. It is also a selective inhibitor of phosphodiesterase III (PDE3). Apremilast, a novel PDE4 inhibitor, inhibits spontaneous production of tumour necrosis factor-alpha from human rheumatoid synovial cells and ameliorates experimental arthritis. *Available package size: 2,5,10,25mg A11326 Bay A12550 A12619 A12776 A13121 A13722 Zardaverine Avanafil AN2728 PF Deltarasin-HCl Deltarasin is a novel small molecule inhibiting the KRAS PDEδ interaction and thus impairing oncogenic KRAS signalling. *Available package size: 5,10,25mg Hydroxylases A10485 A10542 Isotretinoin LX 1606 Hippurate A11058 A11138 Abiraterone Acetate (CB7630) TOK-001 (Galeterone) A10804 A10805 Roflumilast Rolipram Abiraterone (CB-7598) inhibits 17 α-hydroxylase/c17,20 lyase (CYP17A1), an enzyme which is expressed in testicular, adrenal, and prostatic tumor tissues. A10081 A10102 A10120 A10200 A10234 A10498 A10578 A10625 A10853 A10978 A11044 Apigenin Avasimibe (CI-1011) Baicalein Chloramphenicol Clotrimazole Ketoconazole Methoxsalen (Oxsoralen) Naringenin Sodium Danshensu Voriconazole (Vfend) TAK-700 (Orteronel) TOK-001 (Galeterone) is both an androgen receptor antagonist and CYP17A1 inhibitor. A11144 A11277 A11481 A11865 A11977 TH-302 Cobicistat(GS-9350) Luliconazole Hydroxyflutamide TMS A12544 PF A13361 A13365 ABT 3-Cyano-7-ethoxycoumarin A10965 A11019 A11073 A11191 Vardenafil Ibudilast (KC-404) Ibudilast, a pharmacologic phosphodiesterase inhibitor, prevents human immunodeficiency Virus-1 Tat-Mediated activation of microglial cells. *Available package size: 10,50,100mg GSK PF A11289 Apremilast (CC 10004) LX 1606 hippurate is an orally bioavailable, small-molecule, tryptophan hydroxylase (TPH) inhibitor with potential antiserotonergic activity. A10637 Nepicastat (free base) (SYN-117) Nepicastat is an inhibitor of dopamine beta-hydroxylase, an enzyme that catalyzes the conversion of dopamine to norepinephrine.

11 15 Cell Metabolism Cell Metabolism 16 A11172 A11183 Nepicastat hydrochloride PF-3845 Cyclooxygenase (COX) Histone Deacetylase (HDAC) A11785 LX 1606 A12833 Ro A13363 Metyrapone A13998 DMOG Dihydrofolate reductase (DHFR) A10021 Methotrexate (Abitrexate) A10655 NSC (DAMPA) A10707 Pemetrexed (Alimta) A12796 Trimetrexate A10030 A10090 A10193 A10304 A10382 A10461 A10462 A10474 A10623 A10720 A10736 Acetaminophen Asaraldehyde (Asaronaldehyde) Celecoxib Diclofenac sodium Febuxostat (TEI-6720) Ibuprofen (Advil) Ibuprofen Lysine (NeoProfen) Indomethacin (Indocid, Indocin) Naproxen sodium Phenylbutazone Piroxicam (Feldene) NS-398 is a COX-2 inhibitor used in the study of the function of cyclooxygenases. A13244 A13332 FK 3311 A13342 A13572 Bromfenac sodium Valdecoxib Parecoxib A10122 Belinostat (PXD101) Belinostat (PXD101) is a HDAC inhibitor that inhibits HDAC activity in HeLa cell extracts with an IC50 of 27 nm. *Available package size: 10,50,100,200mg A10179 A10246 Carbamazepine CUDC-101 Antimetabolite A10177 Capecitabine (Xeloda) Trimetrexate is a quinazoline derivative. It is a dihydrofolate reductase inhibitor. Dehydrogenases A10780 A11403 A11682 A11786 Ranolazine MK-8245 Gimeracil CPI-613 Piroxicam is an effective and potent inhibitor of prostaglandin synthesis and a Cox-1 and Cox-2 inhibitor. *Available package size: 250,500mg A10749 Pravadoline (WIN 48098) A10878 Sulindac (Clinoril) A11292 Alvimopan (ADL ) A11464 Iguratimod (T 614) A11686 A11692 A11693 A11694 Flunixin meglumine Acemetacin (Emflex) Tolfenamic acid Nimesulide Capecitabine is a prodrug, that is enzymatically converted to 5-fluorouracil in the tumor, where it inhibits DNA synthesis and slows growth of tumor tissue. *Available package size: 1,5g A10183 A10223 A10251 Carmofur Cladribine Flupirtine maleate CUDC-101 is a novel compound which inhibits multiple targets, which is designed to inhibit HDAC, EGFR and Her2. *Available package size: 10,50,100,200mg A10337 A10488 A10492 A10516 Droxinostat ITF2357 (Givinostat) JNJ LAQ824 (NVP-LAQ824) A11695 Lornoxicam (Xefo) A11697 Licofelone CPI-613 is a racemic mixture of the enantiomers of a synthetic alphalipoic lipoic acid analogue with potential chemopreventive and antineoplastic activities. A12385 A12442 A12902 A12903 CGP 3466B maleate Brequinar 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. AGI-6780 A12925 JK 184 Licofelone is a dual COX/LOX inhibitor, being considered as a treatment for osteoarthritis. It may reduce the gastrointestinal toxicity associated with other non-steroidal anti-inflammatory drugs, which only inhibit COX (cyclooxygenase). Licofelone is the first drug to inhibit both. A11906 A11918 A11986 A12434 A13116 Phenacetin Rofecoxib (Vioxx) ATB-337 (S)-(+)-Flurbiprofen NS-398 Flupirtine maleate is a Non-opioid analgesic with muscle relaxant properties. *Available package size: 10,25,100mg A10286 A10292 Daphnetin Decitabine Decitabine is a hypomethylating agent.it hypomethylates DNA by inhibiting DNA methyltransferase. A10395 A10396 Fludarabine Phosphate (Fludara) Fludarabine (Fludara) LAQ824 (NVP-LAQ824) is a potent novel histone deacetylase inhibitor with significant activity against multiple myeloma. *Available package size: 10,50,100mg A10518 A10560 LBH589 (Panobinostat) MC1568 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. A10586 A10611 A10700 MGCD0103 (Mocetinostat) MS-275 (Entinostat) PCI A10764 Pyroxamide (NSC ) A10830 A10947 SB939 Trichostatin-A (TSA)

12 17 Cell Metabolism Cell Metabolism 18 A10954 A10979 A11037 A11042 A11152 Tubacin Vorinostat (SAHA) AR-42 (HDAC-42) Tubastatin A HCl PCI EX 527 is a potent and selective SIRT1 class III histone deacetylase enzyme inhibitor *Available package size: 5,10,25,100mg A10785 A10862 Resveratrol SRT1720 A10158 A10800 A12411 A12518 A12870 BMS Rivaroxaban (Xarelto) Rivaroxaban Diol Betrixaban Razaxaban A11065 CX-5461 A12871 Letaxaban (TAK-442) A13878 ABT333 Kinesin Spindle Protein 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. PCI is a specific and potent histone deacetylase 8 (HDAC8) inhibitor, with >200-fold selectivity over the other HDAC isoforms. A10486 Ispinesib (SB ) A11147 A11179 A11803 CCT NSC (XI-006) Azithromycin (Zithromax) A11153 A11920 CUDC-907 Romidepsin (FK228,Depsipeptide) A11804 A12326 Adenine sulfate INNO-206 (Aldoxorubicin) A11940 ACY-1215 (Rocilinostat) A11964 CI994 (Tacedinaline) SRT1720 is an inhibitor developed intended as a small-molecule activator of the sirtuin subtype SIRT1. *Available package size: 5,10,50,200mg CI-994 is a histone deacetylase (HDAC) inhibitor and induces histone hyperacetylation in living cells. *Available package size: 10,50,100mg A12527 A12904 Monoamine Oxidase (MAO) A10078 A10818 A11722 Inauhzin AK-7 Aniracetam Safinamide Mesylate (FCE28073) Rasagiline mesylate Ispinesib (SB ) is a potent inhibitor of kinesin spindle protein, a kinesin motor protein essential for the formation of a bipolar mitotic spindle and cell cycle progression through mitosis. A10828 SB A11050 Arry-520 A11170 AZ 3146 Aldoxorubicin, also known as INNO-206, is the 6-maleimidocaproyl hydrazone derivative prodrug of the anthracycline antibiotic doxorubicin (DOXO-EMCH) with antineoplastic activity. A12409 Epirubicin A12556 Resminostat Resminostat, also known as RAS2410, is a potent inhibitor of histone deacetylase (HDAC) classes I and II. It binds to and inhibits HDACs leading to an accumulation of highly acetylated histones. A12722 A12745 A12911 A13218 Scriptaid Apicidin BRD9757 RGFP966 Rasagiline is an irreversible inhibitor of monoamine oxidase used as a monotherapy in early Parkinson's disease or as an adjunct therapy in more advanced cases. *Available package size: 50,100mg A11777 A11885 A13294 A13353 Factor Xa A10082 SL Moclobemide Safinamide Bifemelane hydrochloride Apixaban (BMS ) AZ 3146 is a potent and selective monopolar spindle 1 (Mps1) kinase inhibitor (IC50 = 35 nm). It interferes with chromosome alignment and overrides spindle assembly checkpoint and also Inhibits the recruitment of Mad1, Mad2 and centromere protein E (CENP-E) to kinetochores. A11976 DNA, RNA and Protein Synthesis A10036 A10152 A10182 A10221 A10224 Monastrol Cycloheximide (Actidione) Bleomycin sulfate Carboplatin Cisplatin Clafen (Cyclophosphamide) 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). A12890 CYP17 A11044 A11138 Thiostrepton TAK-700 (Orteronel) TOK-001 (Galeterone) Sir2-like Family Deacetylases (sirtuins) A10377 EX 527 A10228 A10281 A10346 A10392 Clofarabine Dacarbazine Oxaliplatin (Eloxatin) Floxuridine Apixaban is an anticoagulant for the prevention of venous thromboembolism and venous thromboembolic events. A10466 A10532 A10568 A10597 Ifosfamide Lincomycin hydrochloride (U-10149A) Mercaptopurine Mizoribine TOK-001 (Galeterone) is both an androgen receptor antagonist and CYP17A1 inhibitor. A10632 Nelarabine (Arranon)

13 19 Cell Metabolism Cell Metabolism 20 A11409 A13515 Cyproterone acetate TAK-700 (salt) A11084 Anacetrapib (MK-0859) A13004 INCB Ferroptosis Phospholipases A10206 A10548 Lipid Metabolism A11230 PF PF is a reversible, competitive inhibitor of sterol regulatory element-binding protein (SREBP) site 1 protease. A11242 A12318 FAAH A11049 Torcetrapib (CP ) SC URB597 URB597 is a relatively selective inhibitor of the enzyme fatty acid amide hydrolase (FAAH). *Available package size: 5,25,50,100mg A12420 JNJ Chlorpromazine hydrochloride LY (Varespladib) LY (Varespladib) is an inhibitor of the IIa, V, and X isoforms of secretory phospholipase A2 (spla2). Anacetrapib (MK-0859) is a CETP inhibitor being developed to treat hypercholesterolemia (elevated cholesterol levels) and prevent cardiovascular disease. A11213 A11397 DNA Methyltransferases A10105 A10292 A12744 Azacitidine(Vidaza) Decitabine SGI-110 HMG-CoA Reductase A10737 Pitavastatin calcium (Livalo) Pitavastatin Calcium is a competitive inhibitor of the enzyme HMGCR (HMG-CoA reductase) results in a reduction in LDL cholesterol synthesis. A11800 A11877 A11912 A13709 A13743 Atorvastatin calcium Neuronal Metabolism A12404 ONO 2506 JTT-705 (Dalcetrapib) Evacetrapib (LY ) Lovastatin (Mevacor) Pravastatin sodium Mevastatin Atorvastatin INCB is an orally available hydroxyamidine and inhibitor of indoleamine 2,3-dioxygenase (IDO1), with potential immunomodulating and antineoplastic activities. Akt A10003 A10094 MK-2206 dihydrochloride AT7867 AT7867 is a novel and potent inhibitor of both AKT and the downstream kinase p70 S6 kinase (p70s6k) and also of protein kinase A. A10453 A10709 A11024 A11030 A11031 A11032 A11033 Honokiol Perifosine (NSC ) PF GSK CCT PHT-427 A11034 A A11246 A11286 Triciribine phosphate (NSC ) GDC-0068 A11287 A A11759 A12877 A13210 AKT inhibitor VIII (AKTI-1/2) AZD5363 KP372-1 Triciribine A12916 A13247 A13822 Ferrostatin-1 (ethyl ester) Ferrostatin-1 (Fer-1) Erastin PI3K / Akt / mtor A13460 PI3-Kinase (PI3K) A10088 A10112 A10133 A10172 A10421 A10438 A10463 Deguelin AS AZD6482 BEZ235 (NVP-BEZ235) CAL-101 (GS-1101) GDC-0941 GSK IC IC was the first isoform-selective PI3K inhibitor: p110m-nm- 4(IC50 = 0.13 M-BM-5M) vs. p110m-nm-1(ic50 = 200 M-BM-5M), p110m-nm-2(ic50 = 16 M-BM-5M) and p110m-nm-3(ic50 = 61 M-BM-5M). *Available package size: 5,10,25,100mg A10547 A10693 LY Palomid 529 (P529) JNJ is a selective and reversible inhibitor of fatty acid amide hydrolase (FAAH) (IC50 = 12nM). CETP ONO 2506 inhibits S100B synthesis in activated cultured astrocytes. IDO Triciribine, also known as API-2, suppresses the phosphorylation level and kinase activity of Akt. Palomid 529 is a dual TORC1/2 inhibitor of the PI3K/Akt/ mtor pathway having broad activity in angiogenesis and cellular proliferation *Available package size: 10,50,100,200mg A10727 A10728 PIK-293 PIK-294

14 21 PI3K / Akt / mtor PI3K / Akt / mtor 22 A Methyladenine A11784 GSK A10746 PP242 A11161 Wortmannin A11956 TG A11162 NVP-BGT226 A12422 IPI-145 A11169 CH A11196 CAY10505 A11197 AS PIK-294 is a PI3 Kinase inhibitor that is 20- to 60-fold more potent than the parent compound, PIK-293. It is one of the most potent p110δ-selective inhibitors that has been reported. A10729 A10730 A10731 A10765 A10766 A10922 PIK-75 PIK-90 PIK-93 Quercetin dihydrate (Sophoretin) Quercetin (Sophoretin) TG AS inhibited MCP-1-mediated monocyte chemotaxis with an IC50 value of 21 µm and reduced RANTES-induced peritoneal neutrophil recruitment in a murine model of leukocyte chemotaxis with an ED50 value of 42.4 mg/kg. A11198 D A11202 A66 IPI-145, also known as INK-1197, is an orally bioavailable, highly selective and potent small molecule inhibitor of the delta and gamma isoforms of phosphoinositide-3 kinase (PI3K) with potential immunomodulating and antineoplastic activities. A12480 A12704 A12831 A12935 VS-5584 SF1126 GDC-0032 PF PP242 is a potent and selective mtor inhibitor in both mtorc1 and mtorc2. A10782 A10906 A10989 Rapamycin (Sirolimus) Temsirolimus (Torisel) WYE-354 A11207 PP121 TG inhibits PI3K γ and -δ(ic50 values of 83 and 235 nm, respectively). *Available package size: 5,10,25,100mg A10923 A10995 A10997 A11014 TGX-221 XL147 XL765 ZSTK474 PP121 is a dual inhibitor of receptor tyrosine kinases (RTKs) (IC50 < 0.02 μm for Abl, Src, VEGFR-2 and PDGFR) and PI 3-K family kinases (IC50 < 0.06 μm for p110α, DNA-PK and mtor). A11261 PX-866 PF is a highly potent and orally bioavailable PI3K/mTOR dual inhibitor. *Available package size: 2,5,10mg A13021 HS-173 A13224 KU A13879 mtor CNX-1351 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. A11038 A11056 A11079 A11187 A11188 WYE (WYE-132) OSI-027 PKI-587 WYE-687 WAY-600 A10114 AZD8055 A11303 AZD2014 ZSTK474 is an ATP-competitive inhibitor of class I phosphatidylinositol 3 kinase isoforms. A11016 A11023 A11035 A11064 A11089 BKM120 (NVP-BKM120) GDC-0980 (RG7422) GSK YM PKI-402 PX-866 is a small-molecule wortmannin analogue inhibitor of the alpha, gamma, and delta isoforms of phosphoinositide 3-kinase (PI3K) with potential antineoplastic activity. A11328 BYL719 AZD8055 is a potent, selective, and orally bioavailable ATPcompetitive mtor kinase inhibitor with an IC50 of 0.8 nm. A10295 A10374 A10505 Deforolimus (Ridaforolimus) Everolimus (RAD001) KU AZD2014 is an orally bioavailable inhibitor of the mammalian target of rapamycin (mtor) with potential antineoplastic activity. mtor kinase inhibitor. A11443 GDC-0349 A11461 INK 128 A11098 NU-7441 (KU-57788) A11099 AS BLY719 is an orally bioavailable phosph-atidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity. AS is a potent inhibitor of PI3K with selectivity for the γ isoform. It inhibits human recombinant PI3Kγ, α, β, and δ with IC50 values of 30, 940, 20,000, and 20,000 nm respectively. A11363 A11511 CZC24832 NVP-BAG956 A11766 BAY KU is a selective inhibitor of mammalian target of rapamycin (mtor) (IC50 ~10 nm for mtorc1 and mtorc2 respectively). *Available package size: 5,25,50,100mg INK 128 is a TORC1/2 inhibitor, is also an orally bioavailable inhibitor of raptor-mtor (TOR complex 1 or TORC1) and rictor-mtor (TOR complex 2 or TORC2) with potential antineoplastic activity.

15 Receptor Tyrosine Kinases 23 PI3K / Akt / mtor 24 A11586 Torin 2 DNA-dependent protein kinase (DNA-PK) A11558 A11752 SU-5402 Lapatinib (free base) A10963 A10967 Vandetanib (ZD6474) Vatalanib (PTK787) 2HCl A10726 PI-103 A11948 A11949 AP26113 AG-17 A10996 A11263 XL184 free base (Cabozantinib) BMS A12448 Butein A11396 E-7050 (Golvatinib) A12650 PKC 412 A11407 Apatinib (YN968D1) A12867 CGP A11496 Motesanib (AMG706) Torin 2 is a potent and selective mtor inhibitor (IC50 = 2.1 nm). Displays 800-fold cellular selectivity for mtor over PI3K (cellular EC50 values are 0.25 and 200 nm for mtor and PI3K respectively). A11587 Torin 1 A11950 A12395 PDK1 A10681 A11148 A11149 Zotarolimus XL388 OSU BX-795 BX-912 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. PI-103 is a potent, cell-permeable, ATP-competitive inhibitor of phosphatidylinositol 3-kinase (PI3K) family members with selectivity toward DNA-PK, PI3K (p110α), and mtor. A11098 Ribosomal S6 protein kinases (RSK) A11160 SL A11423 FMK A11755 PF A12452 NU-7441 (KU-57788) A11778 Compound 401 A12752 NU7026 BI-D1870 A12868 ARRY-543 A13588 Tyrphostin AG 183 A13681 AZD-9291 A13718 Icotinib Hydrochloride A13755 CNX-2006 A13825 Icotinib FGFR A10703 PD A11075 AZD4547 A11159 BGJ398 (NVP-BGJ398) A11244 LY PDGFR A10504 KRN 633 A10880 Sunitinib Malate A10903 Telatinib (BAY ) A11052 Crenolanib (CP ) A11557 A11772 A11954 A11955 A11978 A12027 A12437 A13234 A13377 A13465 A13966 SU14813 CP ZM hydrochloride ZM hydrochloride Delphinidin chloride (-)-Catechin gallate SU 5416 (Semaxinib) SKLB1002 SAR SKLB610 TPT-260 (Dihydrochloride) Type 1 insulin-like growth factor receptor (IGF- 1R) A10440 A10658 A11021 GSK A NVP-ADW742 NVP-AEW541 A11511 NVP-BAG956 A12767 GSK A13484 PS 48 A11350 CP A11581 Toceranib (PHA , SU 11654) A11753 MK-2461 A11978 Delphinidin chloride Receptor Tyrosine Kinases EGFR/HER2 A10702 PD (HCl salt) A10706 Pelitinib (EKB-569) A10043 AEE788 A10990 WZ3146 A10047 AG-490 A10991 WZ4002 A10053 Tyrphostin AG 879 A10992 WZ8040 A10062 AST-6 A11022 AG-1478 (Tyrphostin AG-1478) A10116 AZD8931 A11027 Arry-380 A10141 BIBW2992 (Afatinib) A11028 AV-412 A10210 Chrysophanic acid (Chrysophanol) A11051 PF A10211 Canertinib (CI-1033) A11057 XL647 A10242 CP A11155 AST-1306 A10362 Erlotinib Hydrochloride A11158 ARRY A10422 Gefitinib (Iressa) A11209 BMS (AC480) A10514 Lapatinib Ditosylate A11236 TAK-285 A10612 Mubritinib (TAK 165) A11263 BMS A10638 Neratinib (HKI-272) A11334 BIBX 1382 A10678 OSI-420 A11407 Apatinib (YN968D1) VEGFR A10025 Linifanib (ABT-869) A10049 Albendazole A10101 Tivozanib (AV-951) A10103 Axitinib A10137 Bibf1120 (Vargatef) A10162 Brivanib alaninate (BMS ) A10185 Cediranib (AZD2171) A10204 Chloroxine A10248 CYC116 A10254 Brivanib (BMS ) A10259 Imatinib (Gleevec) A10340 E7080 (Lenvatinib) A10495 Kaempferol A10502 Ki8751 A10504 KRN 633 A10608 Motesanib Diphosphate (AMG-706) A10699 Pazopanib Hydrochloride (GW786034) A10893 Taxifolin A10953 TSU-68 (SU6668) NVP-AEW541 is a selective IGF-1R kinase inhibitor that inhibits the autophosphorylation activity of IGF-1R (IC50 = um) and prevents IGF-1-mediated survival and proliferation of MCF-7 cells (IC50 = 0.16 and 1.64 um, respectively). *Available package size: 2,5,10,25mg A11053 OSI-906 OSI-906 is a potential first-in-class selective small molecule, dual kinase inhibitor of both insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR). A11054 A11059 A11400 BMS BMS A11951 PQ 401 A12195 A13069 AG-1024 (Tyrphostin) Picropodophyllin XL-228