InSolution Y-27632-Calbiochem

C₁₄H₂₁N₃O · 2HCl · xH₂O

320.26 (anhydrous basis)

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 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).

Target IC₅₀: 700 nM against phenylephrine-induced contractions in aortic strips
Cell permeable: yes
Target K_i: 140 nM for p160ROCK (ROCK-I)
Reversible: no
Product competes with ATP.
Primary Target
p160ROCK

Toxicity: Harmful (C)

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

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

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.

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

100

≥95% (HPLC)

liquid

Calbiochem^®

OK to freeze
protect from light

wet ice

−20℃

500 μg in Plastic ampoule
Packaged under inert gas

12 - Non Combustible Liquids

WGK 2