Y-27632 is a highly potent, cell permeable, selective and ATP competitive inhibitor of ROCK1 and ROCK2 (IC50=800nM). It acts as a potent inhibitor of agonist-induced Ca²⁺sensitization of myosin phosphorylation and smooth muscle contractions, blocking cell spreading and suppresses RhoA-induced formation of stress fibers in hepatic stellate cells. Y-27632 significantly reduces the increase of inflammatory cytokines after reperfusion, preventing the development of acute renal failure. There are numerous application for this compound including: cardioprotective effects, suppression of tumor cell invasion, inhibition of superoxide production, mimicking effect of β-agonists on human cells, and an antinociceptive effect.
 
There has been a growing interest in Y-27632 for use in stem cell self-renewal and reprogramming. It is known to increase the survival rate of human embryonic stem cells undergoing cryopreservation.