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BDP5290

Catalog No. T7301 CAS 1817698-21-7

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.)

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BDP5290, CAS 1817698-21-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 51.00
2 mg	In stock	$ 74.00
5 mg	In stock	$ 122.00
10 mg	In stock	$ 198.00
25 mg	In stock	$ 409.00
50 mg	In stock	$ 595.00
100 mg	In stock	$ 866.00
1 mL * 10 mM (in DMSO)	In stock	$ 133.00

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Purity: 98%

Biological Description

Chemical Properties

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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.
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.

Molecular Weight	371.82
Formula	C17H18ClN7O
CAS No.	1817698-21-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 12.5 mg/mL (33.62 mM)

References and Literature

1. Unbekandt M , Croft D R , Crighton D , et al. A novel small-molecule MRCK inhibitor blocks cancer cell invasion[J]. Cell Communication and Signaling, 2014, 12(1):54.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library TGF-beta/Smad Compound Library Bioactive Compound Library Kinase Inhibitor Library Bioactive Compounds Library Max Cytoskeletal Signaling Pathway Compound Library Anti-Cancer Compound Library Reprogramming Compound Library Stem Cell Differentiation Compound Library Cell Cycle Compound Library

Related Products

Related compounds with same targets

ROCK-IN-1 Cucurbitacin A ROCK2-IN-6 hydrochloride WAY-656935 SB-772077B dihydrochloride LX7101 SR-3677 CKI-7

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

BDP5290 1817698-21-7 Cell Cycle/Checkpoint Cytoskeletal Signaling Stem Cells ROCK inhibit Rho-kinase BDP-5290 Rho-associated kinase Rho-associated protein kinase ROK BDP 5290 Inhibitor inhibitor

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