RKI-1447 is an inhibitor of the Rho-associated kinases ROCK1 and 2 (IC50s = 14.5 and 6.2 nM, respectively) that functions by binding to the ATP binding site of the kinase. In cancer cells, RKI-1447 at a concentration of 100 nM has been found to suppress the activation of ROCK substrates myosin light chain (MLC)-2 and the MLC phosphatase PP1 regulatory subunit MYPT1 without effect on the phosphorylation of Akt, MEK, or S6 kinase. Furthermore, it can prevent ROCK-mediated migration, invasion, and anchorage-independent growth of MDA-MB-231 breast cancer cells (IC50 = 709 nM).
[1] patel r a et al. , rki-1447 is a potent inhibitor of the rho-associated rock kinases with anti-invasive and antitumor activities in breast cancer. cancer res, 2012, 72(19): 5025-5034.
