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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.1 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.1 Furthermore, it can prevent ROCK-mediated migration, invasion, and anchorage-independent growth of MDA-MB-231 breast cancer cells (IC50 = 709 nM).1
WARNING This product is not for human or veterinary use.
1. RKI-