Chemical Structure : RKI-1447
CAS No.: 1342278-01-6
货号: PC-38732Not 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.
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
10 mg | ¥980 | In stock | |
25 mg | ¥1580 | In stock | |
50 mg | ¥2580 | 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.
分子量 | 326.374 | |
分子式 | C16H14N4O2S | |
外观性状 | Solid | |
储存条件 |
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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 |
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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