BDP5290

BDP5290 is a potent inhibitor of ROCK and MRCK with IC50 values of 17nM, 230nM, 123nM and 100nM for MRCKβ, ROCK1, ROCK2, respectively .

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2mg

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5mg

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Background

BDP5290 is a potent inhibitor of ROCK and MRCK with IC50 values of 17nM, 230nM, 123nM and 100nM for MRCKβ, ROCK1, ROCK2, respectively ^[1].

BDP5290 (2 μM, 24h) treated ATII cells decreased baseline TEER, and prevented the β1 subunit-induced increase of barrier integrity ^[2]. 3 μM BDP5290 completely inhibited MLC phosphorylation induced by MRCKβ, but not by ROCK1 or ROCK2 ^[1]. BDP5290 treated parental MDA-MB-231 breast cancer cells at varying concentrations, and showed endogenous MRCK and ROCK inhibition effect of pMLC with EC50 of 316 nM ^[1]. application of 0.5 μM BDP5290 lessened both cytoplasmic and cortical pMLC levels in MDA-MB-231 cells ^[1]. BDP5290 reduced MDA-MB-231 invasion at concentrations starting from 0.1 μM, with virtually complete inhibition at 10 μM ^[1]. 2-μM BDP5290 strongly inhibited the ability of human SCC12 squamous cell carcinoma cells to invade a 3D collagen matrix ^[1].

参考文献:
[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): 1-15.
[2]. Bai H, Zhou R, Barravecchia M, et al. The Na+, K+-ATPase β1 subunit regulates epithelial tight junctions via MRCKα[J]. JCI insight, 2021, 6(4).

Protocol

Cell experiment [1]:
Cell lines	Alveolar epithelial type II cells (ATII)
Preparation Method	ATII cells were cotransfected with plasmids (CMV-tet and Tet-β1) 24 hours after isolation and treated immediately with 2 μM MRCKα inhibitor BDP5290. transepithelial electrical resistance (TEER) was measured 24 hours later.
Reaction Conditions	2 μM for 24 hours
Applications	Consistent with siRNA silencing, baseline TEER was decreased upon MRCKα inhibition. BDP5290 treatment prevented the β1 subunit-induced increase of barrier integrity
参考文献: [1]: Bai H, Zhou R, Barravecchia M, et al. The Na+, K+-ATPase β1 subunit regulates epithelial tight junctions via MRCKα[J]. JCI insight, 2021, 6(4).