BDP5290 HCl is a MRCK inhibitor.
CAS Number: 1817698-21-7
Molecular Weight: 408.29
Chemical Name: 4-Chloro-1-(4-piperidyl)-N-[5-(2-pyridyl)-1H-pyrazol-4-yl]pyrazole-3-carboxamide Hydrochloride
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
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.
- Unbekandt M, et al. A novel small-molecule MRCK inhibitor blocks cancer cell invasion. Cell Commun Signal. 2014 Oct 5;12:54.
Products are for research use only. Not for human use.
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