324878
Focal Adhesion Kinase Inhibitor II
The Focal Adhesion Kinase Inhibitor II, also referenced under CAS 869288-64-2, controls the biological activity of Focal Adhesion Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
别名:
Focal Adhesion Kinase Inhibitor II, PF-573,228, PF-228, 6-((4-((3-(Methanesulfonyl)benzyl)amino)-5-trifluoromethylpyrimidin-2-yl)amino)-3,4-dihydro-1H-quinolin-2-one, FAK Inhibitor II, Cdk7 Inhibitor V
InChI
1S/C22H20F3N5O3S/c1-34(32,33)16-4-2-3-13(9-16)11-26-20-17(22(23,24)25)12-27-21(30-20)28-15-6-7-18-14(10-15)5-8-19(31)29-18/h2-4,6-7,9-10,12H,5,8,11H2,1H3,(H,29,31)(H2,26,27,28,30)
InChI key
HESLKTSGTIBHJU-UHFFFAOYSA-N
assay
≥97% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
color
off-white
solubility
DMSO: 50 mg/mL
shipped in
ambient
Quality Level
General description
A cell-permeable pyrimidinyldiamino compound that acts as a selective, ATP-competitive, and potent FAK inhibitor (IC50 = 4 nM). It inhibits CDK7/cycH/MAT1 and CDK1/cycB only at much higher concentrations (IC50 = 197 and 486 nM, respectively) and exhibits little or much reduced activity against 39 other commonly studied kinases (≤64% inhibition at 1 µM). PF-573,228 effectively inhibits cellular FAK Tyr397 phosphorylation in various human, rat, and canine cell lines (IC50 = ~30-500 nM during an 1 h incubation period) and concomitant blockage of Tyr31 phosphorylation of the FAK downstream substrate paxillin is also demonstrated in rat fibroblast REF52 cultures. A useful tool for studying FAK-mediated cellular functions.
Other Notes
Slack-Davis, J.K., et al. 2007. J. Biol. Chem.282, 14845.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
No data available
flash_point_c
No data available
Chien-Chung Huang et al.
Cells, 10(8) (2021-08-28)
Angiogenesis is a critical process in the formation of new capillaries and a key participant in rheumatoid arthritis (RA) pathogenesis. Vascular endothelial growth factor (VEGF) stimulation of endothelial progenitor cells (EPCs) facilitates angiogenesis and the progression of RA. Phosphorylation of
Lohit Khera et al.
Life science alliance, 4(6) (2021-04-01)
Cancer stem cells (CSCs) are implicated in tumor initiation, metastasis and drug resistance, and considered as attractive targets for cancer therapy. Here we identified a clinically relevant signaling nexus mediated by AXL receptor, PYK2 and PKCα and show its impact
我们的科学家团队拥有各种研究领域经验，包括生命科学、材料科学、化学合成、色谱、分析及许多其他领域.
联系客户支持