Inhibitor SourceBook™ Second Edition

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Phosphorylation/Dephosphorylation Protein Tyrosine Kinase (PTK) Inhibitors, continued Product Cat. No. Comments Size Price Radicicol, Diheterospora chlamydosporia 553400 Inhibitor of p60 v-src kinase activity (IC 50 = 8.2 mM). Also inhibits tyrosine phosphorylation of p53/56 lyn in LPS-stimulated macrophages. RG- 3022 554725 [a-(3´-Pyridyl)-(3,4-dimethoxy)cinnamonitrile] A selective inhibitor of EGFR kinase activity. Inhibits epidermal growth factor- stimulated HER 4 cell proliferation (IC 50 = mM) and tumor growth in vivo. Src Kinase Inhibitor I 567805 [4-(4´-Phenoxyanilino)-6,7-dimethoxyquinazoline] A potent, selective, dual site, competitive inhibitor of Src tyrosine kinase (IC 50 = 44 nM and 88 nM for Src and Lck, respectively). Shown to simultaneously interact with both the ATP- and peptide-binding sites. Inhibits VEGFR2 and c-fms tyrosine kinases only at higher concentrations (IC 50 = 320 nM and 30 mM, respectively). Src Kinase Inhibitor II 567806 A potent, selective, and ATP-competitive inhibitor of Src family tyrosine kinases (IC 50 = .2 mM for human recombinant Csk). ST638 567790 [a-Cyano-(3-ethoxy-4-hydroxy-5-phenylthiomethyl)cinnamide] Protein tyrosine kinase inhibitor (IC 50 = 370 nM) that also inhibits HGF-induced MAP kinase activation in hepatocytes. SU 498 572888 {(E)-3-(3,5-Diisopropyl-4-hydroxyphenyl)-2-[(3-phenyl-n-propyl) amino-carbonyl]acrylonitrile} A potent and selective inhibitor of Flk- kinase (IC 50 = 700 nM), a vascular endothelial growth factor (VEGF) receptor kinase. Also reduces the expression of ets-1, a transcription factor stimulated by VEGF. Has only a weak inhibitory effect on PDGFreceptor (IC 50 > 50 mM), EGF-receptor (IC 50 > 00 mM), and HER2 (IC 50 > 00 mM). SU4984 572625 {3[4-(1-Formylpiperazin-4-yl)benzylidenyl]-2-indolinone} Inhibitor of FGFR tyrosine kinase activity (IC 50 = 0–20 mM in the presence of mM ATP). Also inhibits aFGF-induced phosphorylation of ERK and ERK2 and tyrosine phosphorylation of PDGF and insulin receptors. Not available for sale in the United States. SU5402 572630 {3-[3-(2-Carboxyethyl)-4-methylpyrrol-2-methylidenyl]-2-indolinone} Inhibits the tyrosine kinase activity of fibroblast growth factor receptor (FGFR ); (IC 50 = 0–20 mM in the presence of mM ATP). Also inhibits aFGF-induced tyrosine phosphorylation of ERK and ERK2 (IC 50 = 0–20 mM). In contrast to SU4984 (Cat. No. 572625), SU5402 is only a weak inhibitor of tyrosine phosphorylation of the PDGF receptor and does not inhibit phosphorylation of the insulin receptor. Does not inhibit the kinase activity of the EGF receptor. Not available for sale in the United States. SU56 4 572632 {5-Chloro-3-[(3,5-dimethylpyrrol-2-yl)methylene]-2-indolinone} Potent inhibitor of VEGFR kinase, Flk- (IC 50 = .2 mM), and PDGFR kinase (IC 50 = 2.9 mM). Not available for sale in the United States. 500 mg $75 5 mg $ 03 mg $ 03 5 mg $ 52 5 mg $ 28 5 mg $ 23 mg — 500 mg — mg — SU6656 572635 A potent Src family kinase inhibitor. Inhibits Src (IC = 280 nM) and closely related 50 kinases Fyn (IC = 70 nM) and Yes (IC = 20 nM). Also inhibits Lyn (IC = 30 nM), 50 50 50 but only weakly inhibits Lck (IC = 688 mM) and PDGFR (IC > 0 mM). 50 50 mg $ 27 N InSolution SU6656 572636 A 0 mM (500 mg/ 35 ml) solution of SU6656 (Cat. No. 572635) in DMSO. 500 mg $84 N SU 652 572660 {5-[(Z)-(5-Chloro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-N- [2-(diethylamino)ethyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide} A cell-permeable, pyrrole-indolinone compound that acts as a potent and ATPcompetitive tyrosine kinase receptor and angiogenic inhibitor that exhibits greater selectivity for PDGFRb (IC 50 = 3 nM), VEGFR2 (IC 50 = 27 nM), FGFR (IC 50 = 70 nM), and Kit family members (IC 50 = ~ 0–500 nM) over EGFR (IC 50 = > 20 mM). Syk Inhibitor 574711 [3-(1-Methyl-1H-indol-3-yl-methylene)-2-oxo-2,3-dihydro-1H-indole-5-sulfonamide; Spleen Tyrosine Kinase Inhibitor] A cell-permeable, potent inhibitor of Syk (IC 50 = 4 nM). N Syk Inhibitor II 574712 2-(2-Aminoethylamino)-4-(3-trifluoromethylanilino)-pyrimidine-5-carboxamide, Dihydrochloride A cell-permeable pyrimidine-carboxamide compound that acts as a potent, selective and ATP-competitive inhibitor of Syk (IC 50 = 4 nM), and blocks 5-HT release from stimulated RBL-2H3 cells (IC 50 = 460 nM). 500 mg $ 42 5 mg $ 05 mg $75 52 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 TGF-b RI Kinase Inhibitor N TGF-b RI Kinase Inhibitor II 616451 {ALK5 Inhibitor I; [3-(Pyridin-2-yl)-4-(4-quinonyl)]-1H-pyrazole; TbR-I Inhibitor; Transforming Growth Factor-b Type I Receptor Kinase Inhibitor} A cell-permeable, potent, selective, ATP-competitive inhibitor of TGF-b type I receptor tyrosine kinase (IC 50 = 5 nM). Displays ~ 5-fold greater selectivity over p38a MAP kinase (IC 50 = 740 nM). 616452 [ALK5 Inhibitor II; 2-(3-(6-Methylpyridin-2-yl)-1H-pyrazol-4-yl)-1,5-naphthyridine; Transforming Growth Factor-b Type I Receptor Kinase Inhibitor II] A cell-permeable naphthyridinyl pyrazolo compound that acts as a potent, selective, and ATP-competitive inhibitor of TGF-b type I receptor (ALK5; IC 50 = 23 nM, 4 nM, and 8 nM for ALK5 binding, ALK5 auto-phosphorylation and TGF-b cellular assay in HepG2 cells, respectively). Minimally affects a panel of nine closely related kinases including p38 MAPK at IC 50 > 6 mM. 2´-Thioadenosine 589400 (PD 157432) A potent, selective, and irreversible inhibitor of the ErbB subfamily of protein tyrosine kinases. Inactivates ErbB by modifying Cys 797 at the active site. Also inhibits ErbB2 (IC 50 = 45 mM). (-)-Terreic Acid, Synthetic 581810 {(1R,6S)-3-Hydroxy-4-methyl-7-oxabicyclo[4.1.0]hept-3-ene-2,5-dione} A cell-permeable, selective inhibitor of Bruton’s tyrosine kinase (BTK; IC 50 = 0 mM and 3 mM for the basal and activation levels), both in vitro and in vivo. N TrkA Inhibitor 648450 An oxindole compound that acts as a potent and highly selective inhibitor of TrkA (IC 50 = 6 nM), presumably by targeting the ATP-binding pocket of the kinase. Shown to exhibit ≥ 00-fold selectivity over c-fms, Cdk , Cdk2, Itk, JNK-3, p38, PDHK4, c-Raf , Src, UL 3, and VEGFR2. TX- 23 655200 [2-((3,5-di-tert-Butyl-4-hydroxyphenyl)-methylene)-4-cyclopentene-1,3-dione] A cell-permeable inhibitor for Src, eEF2 kinase, and PKA (IC 50 = 2.2, 3.2, and 9.6 mM, respectively). Inhibits EGFR kinase and PKC only at much higher concentrations (IC 50 = 320 mM). N Tyrene CR4 655230 A cell-permeable hydroxystryrylacrylonitrile compound that potently inhibits the kinase activities of JAK2 and Bcr-Abl (IC 50 ~ 00–600 nM and 500–700 nM, respectively), and displays selectivity over other related kinases, namely, Btk, Lck, Lyn, Src, Syk, and ZAP-70 (IC 50 > 5 mM). Tyrosine-Specific Protein Kinase Inhibitor VEGF Receptor Tyrosine Kinase Inhibitor N VEGF Receptor Tyrosine Kinase Inhibitor II VEGF Receptor 2 Kinase Inhibitor I VEGF Receptor 2 Kinase Inhibitor II VEGF Receptor 2 Kinase Inhibitor III N InSolution VEGF Receptor 2 Kinase Inhibitor III 657015 (p60 v-src 137-157 Inhibitor Peptide; VAPSDSIQAEEWYFGKITRRE) Inhibits p60 v-src (IC 50 = 7.5 mM) and epidermal growth factor receptor kinase. 676475 {4-[(4´-Chloro-2´-fluoro)phenylamino]-6,7-dimethoxyquinazoline} A potent inhibitor of vascular endothelial growth factor (VEGF) receptor (Flt and KDR) tyrosine kinase activity (IC 50 = 2.0 mM and 00 nM for Flt and KDR, respectively). 676481 {N-(4-Chlorophenyl)-2-[(pyridin-4-ylmethyl)amino]benzamide} Shown to potently inhibit the kinase activities of KDR, Flt- , and c-Kit (IC 50 = 20 nM, 80 nM, and 240 nM, respectively), and minimally inhibit c-Src and EGF-R activities (IC 50 = 7.0 mM and 7.3 mM). Further, inactive towards the inhibition of CDK- , c-Met, IGF- R, and PKA (IC 50 > 0 mM). 676480 {(Z)-3-[(2,4-Dimethyl-3-(ethoxycarbonyl)pyrrol-5-yl)methylidenyl]indolin-2-one} A highly selective, cell-permeable indolin-2-one class of receptor tyrosine kinase inhibitor (IC 50 = 70 nM) for murine vascular endothelial growth factor receptor 2 (VEGF- R2; KDR/Flk- ). The inhibition is suggested to be competitive with respect to ATP. 676485 [(Z)-5-Bromo-3-(4,5,6,7-tetrahydro-1H-indol-2-ylmethylene)-1,3-dihydroindol-2-one] A cell-permeable receptor tyrosine kinase (RTK) inhibitor [IC 50 = 70 nM for VEGF-R2 (KDR/Flk- ), 920 nM for PDGF-Rb, 4.92 mM for p60 c-src , and 3.3 mM for FGF-R ]. The inhibition is suggested to be competitive with respect to ATP. 676487 {3-[(2,4-Dimethylpyrrol-5-yl)methylidene]-indolin-2-one; SU5416} A cell-permeable, selective, ATP-competitive inhibitor of VEGF-R (KDR/Flk- ) and PDGFR kinases (IC 50 = mM and 20 mM, respectively in NIH-3T3 cells overexpressing Flk- ; K m = 530 nM for ATP). 676498 A 0 mM (500 mg/2 0 ml) solution of VEGF Receptor 2 Kinase Inhibitor III (Cat. No. 676487) in DMSO. 5 mg $ 05 mg $98 2 mg $ 29 2 mg $ 03 mg $ 00 0 mg $90 5 mg $82 500 mg $204 mg $85 5 mg $ 29 mg $99 mg $99 mg $ 8 500 mg $73 Technical Support Phone 800 628 8470 E-mail calbiochem@emdbiosciences.com 53
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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 and 48: Protein Tyrosine Kinase (PTK) Inhib
Page 53: 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
Page 99 and 100: Amyloidogenesis Inhibitors Calbioch
Page 101 and 102: Secretase Inhibitors Deposition of
Page 103 and 104: Secretase Inhibitors Calbiochem •
Page 105 and 106:
Calbiochem • Inhibitor SourceBook
Page 107 and 108:
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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