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Description

A highly potent, cell-permeable, reversible, and selective inhibitor of Rho-associated protein kinases (Ki = 140 nM for p160ROCK). Also inhibits ROCK-II with equal potency. The inhibition is competitive with respect to ATP. Exhibits 10- to 50-fold lower affinity for PKCepsilon than p160ROCK. Does not affect the activity of p21-activated protein kinase (PAK) even at higher concentrations (~100 µ,M). Also acts as a potent inhibitor of agonist-induced Ca2+ sensitization of myosin phosphorylation and smooth muscle contraction. Prevents apoptosis and enhances the survival and cloning efficiency of dissociated hES cells without affecting their pluripotency. Pretreatment with Y-27632 reduces the risk of lung injury in rat models of sepsis. A 5 mM (500 µ,g/296 µ,l) solution of Y-27632 (Cat. No. 688001) in H2O and a 10 mM solution in DMSO (Cat. No. 688002) are also available., A highly potent, cell-permeable, reversible, and selective inhibitor of Rho-associated protein kinase (Ki = 140 nM for p160ROCK (ROCK-I). Also inhibits ROCK-II with almost equal potency. Inhibition is achieved by competing with ATP for binding to the catalytic site. Exhibits 10- to 50-fold lower affinity for PKCepsilon than p160ROCK. Does not affect the activity of p21-activated protein kinase (PAK) even at high concentrations (~100 µ,M). Also acts as a potent inhibitor of agonist-induced Ca2+ sensitization of myosin phosphorylation and smooth muscle contractions (IC50 = 700 nM for phenylephrine-induced contractions in aortic strips). Prevents apoptosis and enhances the survival and cloning efficiency of dissociated hES cells without affecting their pluripotency. Pretreatment with Y-27632 reduces the risk of lung injury in rat models of sepsis.