Biochem/physiol Actions

Reversible: no

Primary Targetp160ROCK

Product competes with ATP.

Target K_i: 140 nM for p160ROCK (ROCK-I)

Cell permeable: yes

Target IC₅₀: 700 nM against phenylephrine-induced contractions in aortic strips

General description

A 5 mM (500 µg/296 µl) aqueous solution of Y-27632 (Cat. No. 688000). A highly potent, cell-permeable, selective inhibitor of Rho-associated protein kinase (K_i = 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 mM). 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).

A highly potent, cell-permeable, selective inhibitor of Rho-associated protein kinase (K_i = 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 mM). 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).

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

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. 1999. J. Cell Biol.141, 1625.Maekawa, M., et al. 1999. Science285, 895.Uehata, M., et al. 1997. Nature389, 990.

Packaging

Packaged under inert gas

500 µg in Plastic ampoule

Physical form

A 5 mM (500 µg/296 µl) solution of Y-27632 (Cat. No. 688000) in H₂O.

Reconstitution

Following initial thaw, aliquot and freeze (-20°C).

Warning

Toxicity: Harmful (C)