Inhibitor SourceBook™ Second Edition

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
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