Potent and selective ROCK inhibitor (IC50
values are 6.2 and 14.5 nM for ROCK2 and ROCK1 respectively); suppresses phosphorylation of ROCK substrates MLC-2 and MYPT-1 in human cancer cells, but has no effect on the phosphorylation levels of Akt, MEK, and S6 kinase. Displays anti-invasive and antitumor activities in breast cancer cells.
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RKI-1447 is a potent inhibitor of the Rho-associated ROCK kinases with anti-invasive and antitumor activities in breast cancer.
Patel et al.
Cancer Res., 2012;72:5025
Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2)
Pireddu et al.