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.)
| Pack Size | Availability | Price/USD | Quantity |
|---|---|---|---|
| 2 mg | In stock | $ 133 | |
| 4 mg | In stock | $ 226 | |
| 8 mg | In stock | $ 361 | |
| 20 mg | In stock | $ 644 | |
| 40 mg | In stock | $ 1023 |
| 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.) |
| Targets&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. |
| CAS No. | 1817698-21-7 |
| Chemical Formula | C17H18ClN7O |
| Molecular Weight | 371.83 |
| Solubility | DMSO: 12.5 mg/mL (33.62 mM) |
| Storage | Powder: -20°C for 2 years In solvent: -80°C for 1 year |
In vivo Formulation Calculator (Clear solution)Calculatorbottom
