Y-27632, free base is a novel and specific inhibitor of Rho-associated kinases (p160ROCK). Y-27632, free base is cell permeable and inhibits ROCK-I and ROCK-II (IC50=800 nM) by competing with ATP and on cultured human cells mimics the effects of β-agonists. In Swiss 3T3 cells Y-27632, free base abolished stress fibers but did not affect G1-S phase transition at 10 µM. Y-27632, free base has been used to increase survival of human embryonic stem cells as well as display cardioprotective effects. Y-27632, free base has been observed to act on smooth muscle contractions and myosin phosphorylation by inhibiting agonist induced Ca2+ sensitization as well as K+-induced contractions, in vascular smooth muscle. In rat ascites hepatoma (MM1) cells Y-27632, free base had suppressed, through regulation of focal adhesion and focal adhesion kinase, tumor cell invasion.
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