BDP5290

SKU: orb1299940

Description

BDP5290 is a potent dual ROCK and MRCK inhibitor, exhibiting IC50 values of 5 nM (ROCK1), 50 nM (ROCK2), 10 nM (MRCKa), and 100 nM (MRCKB). This small molecule is a valuable research tool for studying cytoskeletal dynamics, cell motility, and contractility in both cellular and animal models of cancer and fibrosis.

Research Area

Cell Biology, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1817698-21-7
• MW: 371.82
• Purity: 98.00%
• Formula: C₁₇H₁₈ClN₇O
• SMILES: Clc1cn(nc1C(=O)Nc1c[nH]nc1-c1ccccn1)C1CCNCC1
• Target: ROCK
• Solubility: DMSO:12.5 mg/mL (33.62 mM)

Bioactivity

• Target IC50:
  ROCK1:5 nM |ROCK2:50 nM |MRCKβ:100 nM|MRCKα:10 nM
• In Vitro:
  BDP5290 as a potent MRCK inhibitor. X-ray crystallography of the MRCKβ kinase domain in complex with BDP5290 revealed how this ligand interacts with the nucleotide binding pocket. BDP5290 demonstrated marked selectivity for MRCKβ over ROCK1 or ROCK2 for inhibition of myosin II light chain (MLC) phosphorylation in cells. While BDP5290 was able to block MLC phosphorylation at both cytoplasmic actin stress fibres and peripheral cortical actin bundles, the ROCK selective inhibitor Y27632 primarily reduced MLC phosphorylation on stress fibres. BDP5290 was also more effective at reducing MDA-MB-231 breast cancer cell invasion through Matrigel than Y27632.
• Cell Research:
  MDA MB 231 or SCC12 cells were plated in a 96 well plate and cultured for 24 hours. Cells were then cultured for 24 hours in SCC12 medium with DMSO vehicle, 2 μM Y27632 or indicated concentrations of BDP5290 in an IncuCyte ZOOM. Pictures were taken every 3 hours and confluence was measured using the IncuCyte analysis software. AlamarBlue was added to the medium and the cells were cultured for an additional day. Absorbances at 570 nm and at 600 nm were measured to assess cell health.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BDP5290, BDP-5290, BDP 5290, inhibit, Inhibitor, Rho-kinase, Rho-associated kinase, Rho-associated protein kinase, ROCK, ROK

Compound Identifiers

PubChem CID

85325326