RKI-1447 is a potent small molecule inhibitor of ROCK1 and ROCK2, with IC50 of 14.5 nM and 6.2 nM, respectively, and has anti-invasive and antitumor activities.
RKI-1447 is a type I kinase inhibitor that binds ATP binding sites through interactions with hinge regions and DFG motifs. RKI-1447 inhibits phosphorylation of ROCK substrates mLC-2 and MYPT-1 in human cancer cells, but has no effect on phosphorylation levels of AKT, MEK, and S6 kinases at concentrations up to 10 μM. RKI-1447 is also highly selective in inhibiting Rock-mediated cytoskeletal recombination. RKI-1447 inhibits breast cancer cell migration, invasion and anchor-independent tumor growth [1].
体内研究
In transgenic mouse models, RKI-1447 was highly effective in inhibiting breast tumor growth. The inhibitory effect of RKI-1447 on breast tumor growth was 87%, and the breast tumors of mice treated with RKI-1447 were 7.7 times smaller on average than those treated with carrier control [1].
体外研究
RKI-1447 is a type I kinase inhibitor that binds ATP binding sites through interactions with hinge regions and DFG motifs. RKI-1447 inhibits phosphorylation of ROCK substrates mLC-2 and MYPT-1 in human cancer cells, but has no effect on phosphorylation levels of AKT, MEK, and S6 kinases at concentrations up to 10 μM. RKI-1447 is also highly selective in inhibiting Rock-mediated cytoskeletal recombination. RKI-1447 inhibits breast cancer cell migration, invasion and anchor-independent tumor growth [1].
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