RKI-1447 CAS NO.1342278-01-6

RKI-1447 is a potent small molecule inhibitor of ROCK1 and ROCK2.
IC50 Value: 15.4 nM (ROCK1); 6.2 nM (ROCK2) [1]
Target: ROCK1/2
in vitro: RKI-1447 inhibits potently ROCK1 and ROCK2 in a dose-dependent manner with IC50 values of 14.5 nM and 6.2 nM, respectively. RKI-1447 suppressed phosphorylation of the ROCK substrates MLC-2 and MYPT-1 in human cancer cells, but had no effect on the phosphorylation levels of the AKT, MEK, and S6 kinase at concentrations as high as 10 μmol/L. RKI-1447 was also highly selective at inhibiting ROCK-mediated cytoskeleton re-organization (actin stress fiber formation) following LPA stimulation, but does not affect PAK-meditated lamellipodia and filopodia formation following PDGF and Bradykinin stimulation, respectively. RKI-1447 inhibited migration, invasion and anchorage-independent tumor growth of breast cancer cells [1].
in vivo: Mammary tumors were measured beginning at the time of tumor onset and treatment (once a day for 14 days) with vehicle (20% HPCD) or RKI-1447 (200 mpk/day) began when tumor volumes reached 75 to 2,300 mm3. A wide range of tumor volumes was used to ensure that responses were not volume dependent [1].