A ROCK1 and ROCK2 inhibitor
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.
Patel et al (2012) RKI-1447 is a potent inhibitor of the Rho-associated ROCK kinases with anti-invasive and antitumor activities in breast cancer. Cancer Res. 72 5025 PMID:22846914 |Pireddu et al (2013) Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2) Med.Chem.Comm. 3 699 PMID:23275831
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