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Overview
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Background
Y-27632 is a specific inhibitor of Rho-associated kinases (ROCK) family with Ki values of 0.22 μM and 0.30 μM for ROCK1 and ROCK2, respectively.
Y-27632 has shown selectivity of inhibition by comparing their Ki values for other Rho effector kinases, citron kinase and PKN, as well as PKCα. The Ki values of Y-27632 for citron kinase and PKN are least 20-fold higher, and Ki values for PKCα are about 200-fold higher than those for ROCK kinases. In addition, Y-27632 has been reported to inhibit ROCK1 and ROCK2 by competing with ATP for binding to the kinase in HeLa cells. Besides, Y-27632 has also shown the inhibition of stress fibers in Swiss 3T3 cells when the concentration of Y-27632 is 10 μM [1].[1] Ishizaki T1, Uehata M, Tamechika I, Keel J, Nonomura K, Maekawa M, Narumiya S. Pharmacological properties of Y-27632, a specific inhibitor of rho-associated kinases. Mol Pharmacol. 2000 May;57(5):976-83.
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- Properties
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Overview