BDP5290

SKU: orb1220520

Description

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.)

Key Properties

• CAS Number: 1817698-21-7
• MW: 371.82
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₈ClN₇O
• SMILES: Clc1cn(nc1C(=O)Nc1cn[nH]c1-c1ccccn1)C1CCNCC1
• Target: ROCK
• Solubility: DMSO:12.5 mg/mL (33.62 mM)

Bioactivity

• In Vitro:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

ROCK