BDP5290

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BDP5290 是 ROCK 和 MRCK 的有效抑制剂（ROCK1、ROCK2、MRCKα 和 MRCKβ 的 IC50 值分别为 5 nM、50 nM、10 nM 和 100 nM。）

BDP5290 is a potent inhibitor of both ROCK and MRCK(IC50s of 5 nM 50 nM 10 nM and 100 nM for ROCK1 ROCK2 MRCKα and MRCKβ respectively.)

The Ki of BDP5290 for MRCKα is 10 nM, which is slightly more than the Ki of 4 nM for MRCKβ. 3 μM BDP5290 completely inhibits myosin II light chain (MLC) phosphorylation induced by MRCKβ, but not by ROCK1 or ROCK2. At higher concentrations, BDP5290 reduces MLC phosphorylation (pMLC) to undetectable levels. BDP5290 reduces MDA-MB-231 invasion at all tested concentrations starting from 0.1 μM, with virtually complete inhibition at 10 μM. After 24 hours in the presence of BDP5290 cell viability is slightly reduced with an EC50 ?>10 μM. Wound closure is inhibited by?>60% at 1 μM BDP5290, a concentration that has no effect on cell viability.

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Cell Cycle/DNA Damage

ROCK

ROCK

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1817698-21-7

371.82

C17H18ClN7O

>98% (HPLC)

DMSO:12.5 mg/mL (33.62 mM)

Clc1cn(nc1C(=O)Nc1cn[nH]c1-c1ccccn1)C1CCNCC1

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(-20℃)

With Ice Pack

≥ 2 years