GSK429286A

Description: GSK429286A (also known as RHO15; GSK 429286A; RHO-15; GSK-429286A) is a potent, orally bioactive, and selective inhibitor of ROCK1/2 with antihypertensive effects. It inhibits ROCK1/2 with IC50s of 14 nM and 63 nM, respectively. It reverses adrenalin-induced contraction of the rat aortic ring (IC50 = 190 nM) and causes a dose-dependent decrease in mean arterial blood pressure in spontaneous hypertensive rats. It is shown that GSK429286A treatment (10 uM) increased MYPT phosphrylation at Thr850 via inhibiting ROCK which mediated this phosphorylation process.

References: J Med Chem. 2007 Jan 11; 50(1):6-9.; Biochem J. 2009 Oct 23; 424(1):47-60.