CAY10746

CAY10746 is a selective Rho kinase (ROCK) inhibitor. CAY10746 has inhibitory activity for ROCK I , ROCK II with IC 50 values of 0.014 μM and 0.003 μM, respectively. CAY10746 can be used for the research of diabetic retinopathy (DR)

In Vitro

CAY10746 (compound 12j) has inhibitory activity for ROCK I, ROCK II with IC 50 values of 0.014 μM and 0.003 μM, respectively. CAY10746 (0.1, 1 and 10 μM; 0.25, 1, 2 and 4 h) inhibits ROCK kinase activity in SH-SY5Y cells. CAY10746 (1 μM; 24 h, 36 h) inhibits endothelial cell migration in vitro. CAY10746 (1 μM; 5 days) protects retinal neurons from high glucose-induced oxidative stress and apoptosis-mediated cell death. CAY10746 (1 μM; 5 days) suppresses the improper proliferation of Müller cells and promoted the regression of vascular vessels in retinal explants cultured in a high glucose microenvironment. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: SH-SY5Y cells Concentration: 0.1, 1 and 10 μM; 10 μM Incubation Time: 2 h; 0.25, 1, 2 and 4 h Result: Inhibited the phosphorylation of MYPT1 but did not impact the MYPT1 expression in dose-dependence and time- dependence. Cell Proliferation AssayCell Line: SH-SY5Y cells Concentration: 1 μM Incubation Time: 5 days Result: Significantly protected the cells from death. Cell Migration AssayCell Line: HUVEC cells Concentration: 1 μM Incubation Time: 24 h, 36 h Result: Significantly reduced migrating cell numbers and significantly reduce the rate of wound healing at 24 h and 36 h. Apoptosis AnalysisCell Line: ex vivo DR model Concentration: 1 μM Incubation Time: 5 days Result: Significantly protected neuronal cells from death.

Form:Solid

IC50& Target:IC50: 0.014 μM (ROCK I),0.003 μM (ROCK II)