In vitro
Y-27632, an inhibitor of ROCK (Rho-associated coiled-coil forming protein serine/threonine kinase), can inhibit ROCK by binding to the catalytic site. The inhibition was reversed by ATP in a competitive manner. The Ki value of Y-27632 is at least 20 to 30 times higher than those for two other Rho effector kinases, citron kinase and protein kinase PKN. Y-27632 can abolished stress fibers in Swiss 3T3 cells with 10 uM, without affecting the G(1)-S phase transition of the cell cycle and cytokinesis. Comparing to Y-30141, another ROCK inhibitor, the potency of Y-27632 is 1/10 of that of Y-30141 inhibiting the kinase activity and stress fiber formation. Y-27632 can inhibit migration and morphological change of MM1 cells by suppressing LPA-induced tyrosine phosphorylation of FAK (focal adhesion kinase) and paxillin, which can be regulated by ROCK. Y-27632 dose-dependently inhibited chemotactic and invasive activity of Walker 256 cells s, a rat mammary cancer cell line. Y-27632 also inhibited the phosphorylation level of regulatory myosin light chain in vitro.
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