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Description: RKI-1447 (ROCK Inhibitor XIII; RKI 1447; RKI1447) is a potent small molecule inhibitor of ROCK1 and ROCK2 with potential antitumor activities against breast cancer. It inhibits ROCK1 and ROCK2 with IC50s of 14.5 nM and 6.2 nM, respectively. RKI-1447 is a Type I kinase inhibitor that binds the ATP binding site through interactions with the hinge region and the DFG motif. RKI-1447 suppressed phosphorylation of the ROCK substrates MLC-2 and MYPT-1 in human cancer cells.
References: Cancer Res. 2012 Oct 1; 72(19):5025-34; Medchemcomm. 2012 Jun 1; 3(6):699-709.
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