For research use only. Not for therapeutic Use.
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].
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].
RKI 1447 (200 mg/kg; i.p. daily for 14 days) inhibits mammary tumor growth in vivo[1].
RKI 1447 (100 mg/kg; i.p.; once every 3 days; for 14 days) exerts antitumor activity on CRC in vivo. RKI 1447 does not exert physiological toxicity on the mice[2].
| Catalog Number | I045880 |
| CAS Number | 1782109-09-4 |
| Synonyms | 1-[(3-hydroxyphenyl)methyl]-3-(4-pyridin-4-yl-1,3-thiazol-2-yl)urea;dihydrochloride |
| Molecular Formula | C16H16Cl2N4O2S |
| Purity | ≥95% |
| InChI | InChI=1S/C16H14N4O2S.2ClH/c21-13-3-1-2-11(8-13)9-18-15(22)20-16-19-14(10-23-16)12-4-6-17-7-5-12;;/h1-8,10,21H,9H2,(H2,18,19,20,22);2*1H |
| InChIKey | GBXLRAPHQIRDNS-UHFFFAOYSA-N |
| SMILES | C1=CC(=CC(=C1)O)CNC(=O)NC2=NC(=CS2)C3=CC=NC=C3.Cl.Cl |
| Reference | [1]. Ronil A Patel, et al. RKI-1447 Is a Potent Inhibitor of the Rho-associated ROCK Kinases With Anti-Invasive and Antitumor Activities in Breast Cancer. Cancer Res. 2012 Oct 1;72(19):5025-34. [2]. Liyi Li, et al. RKI-1447 Suppresses Colorectal Carcinoma Cell Growth via Disrupting Cellular Bioenergetics and Mitochondrial Dynamics. J Cell Physiol. 2020 Jan;235(1):254-266. |
