BIX02188

BIX02188 is a selective inhibitor of mitogen-activated protein kinases kinase 5 (MEK5). BIX02188 significantly blocks MEK5 catalytic activity with IC50 of 4.3 nM and inhibits ERK5 catalytic activity with IC50 of 0.81 μM. BIX02188 inhibits transcriptional activation of MEF2C through the MEK5/ERK5 signaling cascade in active MEK5/ERK5/MEF2C-driven luciferase expression system in HeLa and HEK293 cells. BIX02188 also inhibits phosphorylation of BMK1 in bovine lung microvascular endothelial cells (BLMECs) by blocking the MEK5 signal pathway, in a dose-dependent manner with IC50 of 0.8 μM.