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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-ROCK-RKI-1447
RKI-1447

Chemical Structure : RKI-1447

CAS No.: 1342278-01-6

RKI-1447 (RKI1447)

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.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 326.374
分子式 C16H14N4O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-[(3-Hydroxyphenyl)methyl]-N'-[4-(4-pyridinyl)-2-thiazolyl]urea

参考文献

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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