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Y-27632 dihydrochloride
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Not for sale in Japan
Chemical Name:trans-4-[(1R)-1-Aminoethyl]-N-4-pyridinylcyclohexanecar
boxamide dihydrochloride
Biological Activity:
Selective inhibitor of the Rho-associated
protein kinase p160ROCK. Ki values are 0.14, 26, 25 and >250 μM for
p160ROCK, PKC, cAMP-dependent protein kinase and myosin light-chain kinase
respectively. Also inhibits the protein kinase C-related protein kinase, PRK2.
Smooth muscle relaxant and orally active in vivo.
Uehataet al (1997) Calcium sensitization of smooth muscle
mediated by a Rho-associated protein kinase. Nature 389 990. Itohet al (1998) An essential part for Rho-associated kinase in the
transcellular invasion of tumor cells. Nature Med. 5 221. Davieset al (2000) Specificity and mechanism of action of some commonly used
protein kinase inhibitors. Biochem.J. 351 95. Narumiya et al (2000) Use and properties of
ROCK-specific inhibitor Y-27632. Methods Enzymol. 325 273.