Bioactivity | RKI 1447 dihydrochloride is a potent and selective ROCK inhibitor with IC50s of 14.5 and 6.2 nM for ROCK1 and ROCK2, respectively[1]. RKI 1447 dihydrochloride suppresses colorectal carcinoma cell growth and promotes apoptosis[2]. |
Invitro | RKI 1447 suppresses phosphorylation of the ROCK substrates MLC-2 and MYPT-1 in human cancer cells, but has no effect on the phosphorylation levels of the AKT, MEK, and S6 kinase at concentrations as high as 10 μM[1]. RKI 1447 (0.003-10 μM) is potent at inhibiting the phosphorylation of the ROCK substrates MLC-2 and MYPT-1 in human cancer cells[1].RKI 1447 exhibits effective anticancer activity in colorectal carcinoma (CRC). RKI 1447 (10-320 μM; 24 hours) drastically suppresses HCT-8 and HCT-116 cell growth[2]. RKI 1447 (20-80 μM; 24 hours) induces apoptosis in a dose-dependent manner[2]. Cell Viability Assay[2] Cell Line: |
Name | RKI-1447 dihydrochloride |
CAS | 1782109-09-4 |
Formula | C16H16Cl2N4O2S |
Molar Mass | 399.29 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |