In A20 cells, PF-431396 blocks anti-Ig- and clustering LFA-1-induced tyrosine phosphorylation of Pyk2 and FAK, and further blocks B cell spreading. PF-431396 consistently inhibits the increase in protein tyrosine phosphorylation (PY) induced by the absence of added calcium and induced by W-7 in the presence of calcium.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||100 mg/mL in DMSO|
A role for the tyrosine kinase Pyk2 in depolarization-induced contraction of vascular smooth muscle.
Mills RD, et al. J Biol Chem. 2015 Apr 3;290(14):8677-92. PMID: 25713079.
NADPH oxidase/ROS-dependent PYK2 activation is involved in TNF-α-induced matrix metalloproteinase-9 expression in rat heart-derived H9c2 cells.
Yang CM, et al. Toxicol Appl Pharmacol. 2013 Oct 15;272(2):431-42. PMID: 23774252.
|Related FAK Products|
Y15 is a novel small molecule FAK phosphorylation inhibitor; specifically block phosphorylation of Y397-FAK and total phosphorylation of FAK.
PND-1186 (VS-4718) is a reversible and selective FAK inhibitor with IC50 of 1.5 nM.
Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor.
PF-00562271 is the benzenesulfonate salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs.
PF-573228 is an ATP-competitive inhibitor of FAK with IC50 of 4 nM, ~50- to 250-fold selective for FAK than Pyk2, CDK1/7 and GSK-3β.