Product Details
Product Name:
BDP5290 |
CAS No.:
1817698-21-7 |
Purity:
97.22% |
Supply Ability:
10g |
Release date:
2024/11/19 |
Product Introduction
Bioactivity
Name | BDP5290 |
Description | BDP5290 is a potent inhibitor of both ROCK and MRCK, with IC50 values of 5 nM for ROCK1, 50 nM for ROCK2, 10 nM for MRCKα, and 100 nM for MRCKβ. |
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. |
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. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 12.5 mg/mL (33.62 mM)
|
Keywords | inhibit | Rho-kinase | BDP-5290 | Rho-associated kinase | BDP5290 | Rho-associated protein kinase | ROK | BDP 5290 | Inhibitor | ROCK |
Inhibitors Related | SB-747651A Dihydrochloride | GSK180736A | SAR407899 hydrochloride | RKI-1447 | Belumosudil | Fasudil hydrochloride | Y-27632 dihydrochloride | Tofacitinib | Y-27632 | ROCK-IN-5 | Thiazovivin | CAY10746 |
Related Compound Libraries | Neural Regeneration Compound Library | Bioactive Compound Library | Kinase Inhibitor Library | Inhibitor Library | NO PAINS Compound Library | Stem Cell Differentiation Compound Library | Bioactive Compounds Library Max | Cell Cycle Compound Library | Cytoskeletal Signaling Pathway Compound Library | TGF-beta/Smad Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
Product name |
Price |
|
Suppliers |
Update time |
|
$/ |
|
Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |