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].
References:
[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).