Biochem/physiol Actions

Primary Targetp160 Rho-associated protein kinases (ROCK)

Reversible: yes

Product competes with ATP.

Target K_i: 140 nM for p160 Rho-associated protein kinases (ROCK)

Cell permeable: yes

General description

A highly potent, cell-permeable, reversible, and selective inhibitor of Rho-associated protein kinases (K_i = 140 nM for p160^ROCK). Also inhibits ROCK-II with equal potency. The inhibition is competitive with respect to ATP. Exhibits 10- to 50-fold lower affinity for PKC_ε than p160^ROCK. Does not affect the activity of p21-activated protein kinase (PAK) even at higher concentrations (~100 µM). 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 µg/296 µl) 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 p160^ROCK (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 PKC_ε than p160^ROCK. Does not affect the activity of p21-activated protein kinase (PAK) even at high concentrations (~100 µM). 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.

Legal Information

Sold under license of PCT Application W098/06,433A1 and under license from Mitsubishi Pharma Tanabe Corporation.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Cinel, I., et al. 2012. J. Thorac . Dis.4, 30.Watanabe, K., et al. 2007. Nature Biotech.25, 681.Chitaley, K., et al. 2001. Nat. Med.7, 119.Davies, S.P., et al. 2000. Biochem. J. 351, 95.Narumiya, S., et al. 2000. Methods Enzymol.325, 273.Hirose, M., et al. 1998. J. Cell Biol.141, 1625.Maekawa, M., et al. 1999. Science285, 895.Uehata, M., et al. 1997. Nature389, 990.

Packaging

1 mg in Plastic ampoule

Packaged under inert gas

5, 10 mg in Glass bottle

100 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for 6 months at -20°C.

Warning

Toxicity: Harmful (C)