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.)

MRCKβ:100 nM, MRCKα:10 nM , ROCK1:5 nM , ROCK2:50 nM

BDP5290作为一种强效的MRCK抑制剂，通过与MRCKβ激酶域复合的X-射线晶体学研究揭示了该配体如何与核苷酸结合口袋相互作用。BDP5290在抑制细胞中的肌球蛋白II轻链(MLC)磷酸化方面，表现出对MRCKβ较之于ROCK1或ROCK2的显著选择性。而BDP5290能够阻断细胞质肌动蛋白应力纤维和外围皮层肌动蛋白束上的MLC磷酸化，ROCK选择性抑制剂Y27632主要减少了应力纤维上的MLC磷酸化。与Y27632相比，BDP5290在减少MDA-MB-231乳腺癌细胞通过Matrigel侵袭方面也更为有效。

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.