BDP5290 is a potent inhibitor of bothROCKandMRCKwithIC₅₀s of 5 nM, 50 nM, 10 nM and 100 nM forROCK1,ROCK2,MRCKαandMRCKβ, respectively.

The K_iof BDP5290 for MRCKα is 10 nM, which is slightly more than the K_iof 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^[2].

371.82

Solid

C₁₇H₁₈ClN₇O

1817698-21-7

Room temperature in continental US; may vary elsewhere.

DMSO : 12.5 mg/mL(33.62 mM;Need ultrasonic)

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