Inhibitor SourceBook™ Second Edition

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Phosphorylation/Dephosphorylation Protein Tyrosine Kinase (PTK) Inhibitors, continued Due to their involvement in various forms of cancers, PTKs have become prominent targets for therapeutic intervention. Selective receptor and non-receptor PTK inhibitors represent a promising class of anti-tumor agents. These agents are shown to inhibit multiple features of cancer cells, including proliferation, survival, invasion, and angiogenesis. More online... www.calbiochem.com/inhibitors/PTK Protein Tyrosine Kinase (PTK) Inhibitors References: Tibes, R., et al. 2005. Annu. Rev. Pharmacol. Toxicol. 45, 357. Mazitschek, R., Giannis, A. 2004. Curr. Opin. Chem. Biol. 8, 432. Martin, G.S. 200 . Nat. Rev. Mol. Cell Biol. 2, 467. Ghosh, S., et al. 200 . Curr. Cancer Drug Targets 1, 29. Smith, K.M., and Van Etten, R.A. 200 . J. Biol. Chem. 276, 24372. Woodside, D.G., et al. 200 . Curr. Biol. 11, 799. Sada, K. et al. 200 . J. Biochem. (Tokyo) 130, 77. Brasher, B.B., and Van Etten, R.A. 2000. J. Biol. Chem. 275, 3563 . Plattner, R., et al. 999. Genes Dev. 13, 2400. Manes, G., et al. 999. Gene Ther. Mol. Biol. 4, 4 7. Stratowa, C., et al. 999. Anticancer Drug Des. 14, 393. Kyriakis, J.M. 999. J. Biol. Chem. 274, 5259. Product Cat. No. Comments Size Price A77 726 100128 [N-(4-Trifluoromethylphenyl)-2-cyano-3-hydroxycrotoamide] Inhibits the IL-2-induced tyrosine phosphorylation of JAK and JAK3. AG 9 658390 {[(4-Methoxybenzylidene)malononitrile; a-Cyano-(4-methoxy)cinnamonitrile]; Tyrphostin A1} Inactive inhibitor that can be used as a negative control for inhibition of EGFR kinase (IC 50 > 250 mM). AG 7 658425 [a-Cyano-(3,5-di-t-butyl-4-hydroxy)cinnamonitrile; 3,5-di-t-Butyl-4-hydroxybenzylidenemalononitrile; NSC 242557; RG 50872; Tyrphostin A9] A selective inhibitor of the platelet-derived growth factor receptor tyrosine kinase (IC 50 = 500 nM). AG 8 658395 [a-Cyano-(3,4-dihydroxy)cinnamonitrile; RG-50810; Tyrphostin A23] An inhibitor of EGFR autophosphorylation (IC 50 = 40 mM) and the GTPase activity of transducin (IC 50 = 0 mM). AG 30 121760 [a-Cyano-(3,4-dihydroxy)cinnamic Acid; Tyrphostin AG 30] A potent protein tyrosine kinase inhibitor that is specific for c-ErbB. Inhibits the activation of STAT5 by c-ErbB in primary erythroblasts. AG 43 658450 [a-Cyano-(4-hydroxy)dihydrocinnamonitrile; Tyrphostin A63] Useful negative control for tyrphostins (IC 50 = 6.5 mM for EGFR tyrosine kinase activity). AG 82 658400 [a-Cyano-(3,4,5-trihydroxy)cinnamonitrile; Tyrphostin A25] A cell-permeable, competitive inhibitor of substrate binding on protein tyrosine kinases. Inhibits EGFR tyrosine kinase (IC 50 = 3 mM) and the GTPase activity of transducin (IC 50 = 7 mM). AG 99 658430 [a-Cyano-(3,4-dihydroxy)cinnamide; Tyrphostin A46; Tyrphostin B40] An inhibitor of EGFR tyrosine kinase (IC 50 = 0 mM) and EGF-dependent cell proliferation. AG 2 658440 [2-Amino-4-(4´-hydroxyphenyl)-1,1,3-tricyanobuta-1,3-diene; Tyrphostin A48] Inhibits EGFR tyrosine kinase (IC 50 = 25 nM). AG 83 658410 [2-Amino-4-(3´,4´,5´-trihydroxyphenyl)-1,1,3-tricyanobuta-1,3-diene; Tyrphostin A51] An inhibitor of EGFR tyrosine kinase (IC 50 = 800 nM). AG 2 3 658405 [a-Cyano-(3,4-dihydroxy)thiocinnamide; RG-50864; Tyrphostin A47] An inhibitor of EGFR tyrosine kinase (IC 50 = 2.4 mM). AG 490 658401 [a-Cyano-(3,4-dihydroxy)-N-benzylcinnamide; Tyrphostin B42] Potent inhibitor of EGFR kinase autophosphorylation (IC 50 = 00 nM). Also acts as a Jak family tyrosine kinase inhibitor. N AG 490, m-CF 3 658408 [(alpha-cyano-(3,4-dihydroxy)-N-(m-trifluoromethyl)benzylcinnamide] A cell-permeable, m-trifluoromethyl derivative of AG 490 (Cat. No. 65840 ) that displays enhanced antiproliferative properties (IC 50 = .7 mM, 2.8 mM, and 6. mM in 2E8, Baf/3, and Jurkat cells, respectively). Shown to inhibit cytokine-induced JAK kinase activities, and promote cell death. Further, causes significant reductions in lymph node cellularity in IL7TG mouse model ( mg per animal, intraperitoneal). 5 mg $ 00 5 mg $43 5 mg $52 5 mg $52 5 mg $64 5 mg $66 5 mg $52 5 mg $52 5 mg $52 5 mg $90 5 mg $49 5 mg $38 0 mg $88 46 Orders Phone 800 854 34 7 Calbiochem • Inhibitor SourceBook Fax 800 776 0999 Web www.emdbiosciences.com/calbiochem
Protein Tyrosine Kinase (PTK) Inhibitors, continued Calbiochem • Inhibitor SourceBook Phosphorylation/Dephosphorylation Product Cat. No. Comments Size Price AG 494 658407 [a-Cyano-(3,4-dihydroxy)-N-phenylcinnamide; Tyrphostin B48] Inhibitor of EGFR kinase autophosphorylation (IC 50 = .24 mM) that is slightly less active than AG 555 (Cat. No. 658404). AG 527 658402 [a-Cyano-(-)-(R)-N-(a-phenethyl)-3,4-dihydroxycinnamide; (-)-(R)-N- (a-Methylbenzyl)-3,4-dihydroxybenzylidinecyanoacetamide; Tyrphostin B44(-)] An inhibitor of EGFR kinase autophosphorylation (IC 50 = 2.5 mM). Also inhibits the phosphorylation of poly-GAT by the EGF receptor (IC 50 = 400 nM). AG 537, Bis-Tyrphostin 658418 (Bis-Tyrphostin) Competitively inhibits EGFR kinase autophosphorylation (IC 50 = 400 nM). AG 538 658403 [a-Cyano-(3,4-dihydroxy)cinnamoyl-(3´,4´-dihydroxyphenyl)ketone; Tyrphostin AG 538] A potent, competitive inhibitor of insulin-like growth factor- receptor (IGF- R) kinase autophosphorylation (IC 50 = 400 nM). Also inhibits the phosphorylation of PTK substrate poly (Glu,Tyr) by IGF- R, IR, EGF-R, and Src (IC 50 = 60 nM, 3 nM, and 2.4 mM respectively). I-OMe-AG 538 658417 [a-Cyano-(3-methoxy,4-hydroxy,5-iodo)cinnamoyl-(3´,4´-dihydroxyphenyl)ketone; Tyrphostin I-OMe-AG 538] An analog of AG 538 (Cat. No. 658403) that acts as an inhibitor of IGF- receptor kinase both in vitro and in intact cells. Inhibition is competitive with respect to the substrate binding site of IGF- receptor kinase. Exhibits enhanced cell-permeability and increased resistance to oxidation. AG 555 658404 [a-Cyano-(3,4-dihydroxy)-N-(3-phenylpropyl)cinnamide; Tyrphostin B46] A potent inhibitor of EGFR kinase autophosphorylation (IC 50 = 700 nM). Exhibits opposite potency profiles with AG 527 (Cat. No. 658402) for EGF receptor autophosphorylation versus poly-GAT substrate phosphorylation. AG 556 658415 [a-Cyano-(3,4-dihydroxy)-N-(4-phenylbutyl)cinnamide; Tyrphostin B56] A selective inhibitor of EGFR kinase (IC 50 = 5 mM) over HER -2 kinase autophosphorylation. AG 592 658406 {AGL 2592; 2-Cyano-N-(4-{4-[2-cyano-3-(3,4-dihydroxyphenyl)-acryloylamino]cyclohexylmethyl}-cyclohexyl)-3-(3,4-dihydroxyphenyl)-acrylamide} A selective, cell-permeable inhibitor of EGFR-tyrosine kinase activity (IC 50 = 20.3 mM). Blocks thymidine uptake in HER- 4 cells, and displays anti-proliferative properties. AG 825 121765 [4-Hydroxy-3-methoxy-5-(benzothiazolylthiomethyl)benzylidenecyanoacetamide] A potent, selective and ATP-competitive inhibitor of HER-2 (neu/erbB-2, IC 50 = 350 nM) relative to HER- (IC 50 = 9 mM) autophosphorylation. AG 835 658409 [a-Cyano-(+)-(S)-N-(a-phenethyl)-(3,4-dihydroxy)cinnamide; Tyrphostin B50(+)] A less active enantiomer of AG 527 (Cat. No. 658402) that inhibits EGFR kinase poly-GAT (poly-Glu-Ala-Tyr) substrate phosphorylation (IC 50 = 860 nM). AG 879 658460 [a-Cyano-(3,5-di-t-butyl-4-hydroxy)thiocinnamide] An inhibitor of nerve growth factor-dependent pp 40 c-trk tyrosine phosphorylation (EC 50 = 0 mM). Does not affect the tyrosine phosphorylation of EGFR or PDGFR. AG 957 121761 [4-Amino-N-(2,5-dihydroxybenzyl)methyl benzoate; NSC 654705] A potent and selective inhibitor of human p2 0 brc-abl (K i = 750 nM) over p 40 bcr-abl (K i = 0 mM). AG 957, Adamantyl Ester 121762 [4-Amino-N-(2,5-dihydroxybenzyl)adamantyl Benzoate; 4-(2,5-Dihydroxybenzylamino)benzoic Acid Adamantan-1-yl Ester] A lipophilic, adamantyl ester form of tyrphostin AG 957 (Cat. No. 2 76 ) that displays anti-proliferative properties. Shown to be selective and ~3-4 fold more potent than AG 957 as a bcr/abl kinase inhibitor, and also exhibits a longer serum half-life in vivo. AG 024 121767 (3-Bromo-5-t-butyl-4-hydroxy-benzylidenemalonitrile) A specific inhibitor of insulin-like growth factor- (IGF- ) and insulin receptor kinases with significantly lower IC 50 values for IGF- than for insulin receptors. AG 295 658550 (6,7-Dimethyl-2-phenylquinoxaline) A selective inhibitor of PDGFR kinase (IC 50 = 500 nM). Does not affect EGFR autophosphorylation. 5 mg $32 5 mg $33 5 mg $69 5 mg $67 5 mg $67 5 mg $33 5 mg $32 5 mg $ 78 2 mg $93 5 mg $32 5 mg $90 5 mg $92 5 mg $ 84 mg $67 5 mg $87 Technical Support Phone 800 628 8470 E-mail calbiochem@emdbiosciences.com 47
Page 1 and 2: Inhibitor SourceBook Second Editio
Page 3 and 4: Calbiochem • Inhibitor SourceBook
Page 7 and 8: Akt (Protein Kinase B) Inhibitors,
Page 9 and 10: Calmodulin-Dependent Protein Kinase
Page 11 and 12: Casein Kinase (CK) Inhibitors Casei
Page 13 and 14: Checkpoint Kinase Inhibitors Eukary
Page 15 and 16: Cyclin-Dependent Kinase (Cdk) Inhib
Page 21 and 22: Glycogen Synthase Kinase-3 (GSK-3)
Page 23 and 24: Glycogen Synthase Kinase Inhibitors
Page 25 and 26: c-Jun N-Terminal Kinase (JNK/SAP Ki
Page 27 and 28: Mitogen-Activated Protein (MAP) Kin
Page 29 and 30: MAP Kinase Inhibitors, continued Ca
Page 31 and 32: Myosin Light Chain Kinase (MLCK) In
Page 33 and 34: Phosphatidylinositol 3-Kinase (PI 3
Page 37 and 38: Protein Kinase A (PKA; cAMP-Depende
Page 39 and 40: Isozyme Specificities of Selected P
Page 41 and 42: Protein Kinase C (PKC) Inhibitors,
Page 47: Protein Tyrosine Kinase (PTK) Inhib
Page 51 and 52: Protein Tyrosine Kinase (PTK) Inhib
Page 57 and 58: Raf Kinase Inhibitors Raf kinases a
Page 59 and 60: Rho Kinase (ROCK) Inhibitors, conti
Page 61 and 62: Protein Phosphatase Inhibitors Calb
Page 63 and 64: Protein Phosphatase Inhibitors, con
Page 65 and 66: Apoptosis Caspase Inhibitors Activa
Page 67 and 68: Caspase Inhibitors, continued Produ
Page 69 and 70: Other Selected Inhibitors of Apopto
Page 73 and 74: DNA Methyltransferase Inhibitors DN
Page 75 and 76: Histone Acetylase and Deacetylase I
Page 77 and 78: Related Products Histone Deacetylas
Page 79 and 80: Nuclear Import/Export Inhibitors, c
Page 83 and 84: Telomerase Inhibitors, continued Ca
Page 85 and 86: Topoisomerase Related Inhibitors, c
Page 87 and 88: Lipid Signaling Acetyl-CoA Carboxyl
Page 89 and 90: Cyclooxygenase (COX) Inhibitors, co
Page 91 and 92: HMG-CoA (3-Hydroxy-3-Methylglutaryl
Page 93 and 94: Lipoxygenase (LOX) Inhibitors Lipox
Page 95 and 96: Phospholipase Inhibitors Several si
Page 97 and 98: Sphingomyelinase Inhibitors Ceramid
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Amyloidogenesis Inhibitors Calbioch
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Secretase Inhibitors Deposition of
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Secretase Inhibitors Calbiochem •
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Calbiochem • Inhibitor SourceBook
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Glutathione S-Transferase (GST) Inh
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Guanylate Cyclase Inhibitors, conti
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Characteristics of various forms of
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Nitric Oxide Synthase (NOS) Inhibit
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Proteases Anthrax Lethal Factor (LF
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the ratio of active (76 kDa) to ina
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Collagenase Inhibitors (Also see Ma
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Matrix Metalloproteinase (MMP) Inhi
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Matrix Metalloproteinase Inhibitors
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Tissue Inhibitors of Matrix Metallo
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Protease Inhibitors The proper func
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Protease Inhibitors, continued Calb
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Protease Inhibitors, continued Calb
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Protease Inhibitors, continued Sele
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Protease Inhibitor Cocktails, conti
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N Animal-Free Protease Inhibitor Co
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Proteasome and Ubiquitination Pathw
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Transmembrane receptors of various
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Angiotensin-Converting Enzyme (ACE)
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ATPase Inhibitors, continued Calbio
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Calbiochem • Inhibitor SourceBook
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Inhibitors of Glycoprotein Processi
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Heat Shock Protein Inhibitors Heat
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Inhibitors of Mitochondrial Functio
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NF-kB Activation Inhibitors NF-kB,
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NF-kB Activation Inhibitors, contin
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Phosphodiesterase (PDE) Inhibitors
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Plasminogen Activator Inhibitors Ti
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Protein Synthesis Inhibitors, conti
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Sonic Hedgehog Signaling Inhibitors
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Why can’t I make serial dilutions
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Calpastatin, Human, Recombinant, Do
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InSolution Microcystin-LR, Microcys
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RNA Polymerase III Inhibitor ......
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324875 ............................
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Trademarks CALBIOCHEM®
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Your #1 Resource for Inhibitors! We
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