y-27632-2hcl

Description: Y-27632 2HCl (Y27632; Y2 7632), the dihydrochloride salt of Y-27632, is a novel, potent and selective inhibitor of ROCK1 (p160ROCK) with potential antifibrotic and anticancer activity. It inhibits ROCK1 with an IC50 of 140 nM in a cell-free assay, and exhibits > 200-fold selectivity over other closely related kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK. Y27632 prevents dimethylnitrosamine-induced hepatic fibrosis in rats, increases apoptosis and disrupts the actin cortical mat in embryonic avian corneal epithelium, affects initial heart myofibrillogenesis in cultured chick blastoderm, promotes the proliferation and cell cycle progression of cultured astrocyte from spinal cord. Y-27632 suppresses the kinase activity of both ROCK-1 and ROCK-2 in vitro, and this compound inhibits the kinases by binding to the catalytic site of ROCK-1 and ROCK-2. Thus Y-27632 function on Rho-mediated stress fiber formation, the G1-S phase progression and cytokinesis.

Reference: Chin Med J (Engl). 2012 Sep; 125(18):3332-5; Itoh K, et al. Nat Med, 1999, 5(2), 221-225.

Related CAS#: 146986-50-7 (Y27632 free base); 3146986-50-7 (free base); 129830-38-2 (2HCl salt)