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Chemical Structure : RKI 1447 dihydrochloride
CAS No.: 1782109-09-4
Catalog No.: PC-38731Not For Human Use, Lab Use Only.
RKI-1447 is a potent small molecule inhibitor of ROCK1 and ROCK2 with IC50 of 14.5 nM and 6.2 nM, respectively, suppresses phosphorylation of the ROCK substrates MLC-2 and MYPT-1 in human cancer cells.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $98 | In stock | |
| 25 mg | $158 | In stock | |
| 50 mg | $258 | In stock | |
| 100 mg | Get quote |
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RKI-1447 is a potent small molecule inhibitor of ROCK1 and ROCK2 with IC50 of 14.5 nM and 6.2 nM, respectively, suppresses phosphorylation of the ROCK substrates MLC-2 and MYPT-1 in human cancer cells.
RKI-1447 binds the ATP binding site through interactions with the hinge region and the DFG motif.
RKI-1447 shows no effect on the phosphorylation levels of the AKT, MEK, and S6 kinase.
RKI-1447 inhibited migration, invasion and anchorage-independent tumor growth of breast cancer cells (MDA-MB-231 cells, IC50=709 nM).
RKI-1447 is highly effective at inhibiting the outgrowth of mammary tumors in a transgenic mouse model.
| M.Wt | 399.290 | |
| Formula | C16H16Cl2N4O2S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
N-[(3-Hydroxyphenyl)methyl]-N'-[4-(4-pyridinyl)-2-thiazolyl]urea dihydrochloride |
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1. Patel RA, et al. Cancer Res. 2012 Oct 1;72(19):5025-34.
2. Pireddu R, et al. Med Chem Commun. 2012;3(6):699–709.
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