GSK429286A

Data Sheet For research use only. Not for human use.

Cat. No. ：BCP01975CAS No. ：864082-47-3Purity：98%

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CAS No.	864082-47-3	Cat. No.	BCP01975
Name	GSK429286A
Synonyms	GSK 429286 A;GSK-429286A;GSK-429286 A;
SMILES
Chemical Name
Formula	C21H16F4N4O2	M. Wt	432.37
Purity	98%	Storage	Store at 4-8°C
Description	GSK429286A slightly inhibits RSK and p70S6K with IC50 of 0.78 μM and 1.94 μM, respectively. GSK429286A significantly inhibits rat aortic ring dilation with IC50 of 190 nM.GSK429286A at 1 μM reduces ROCK2 activity over 20-fold, under conditions in which the only other kinase tested that is significantly inhibited is MSK1 whose activity is reduced ~5-fold. GSK429286A is a more selective ROCK2 inhibitor than the widely utilized ROCK inhibitor Y-27632 as assessed on kinase-specificity panel, and does not significantly inhibit LRRK2 even at doses as high as 30 μM (500-fold higher than IC50 of inhibition of ROCK2). Like GSK269962A but not sunitinib, GSK429286A treatment at 10 μM ablates basal or G14V-Rho mutant induced phosphorylation of MYPT at Thr850 in HEK-293 cells to a similar extent as H-1152 and Y-27632, consistent with ROCK mediating this phosphorylation, whereas GSK429286A does not inhibit ERM protein phosphorylation either in the presence or absence of G14V-Rho.