BIX02189 is a novel, potent and selective MEK5 inhibitor with an IC50 of 1.5 nM, also inhibits ERK5 catalytic activity with an IC50 of 59 nM. It was reported to inhibit catalytic function of purified, MEK5 enzyme. BIX02189 blocked phosphorylation of ERK5, without affecting phosphorylation of ERK1/2 in sorbitol-stimulated HeLa cells. BIX02189 also inhibited transcriptional activation of MEF2C, a downstream substrate of the MEK5/ERK5 signaling cascade, in a cellular trans-reporter assay system. BIX02189 may offer novel pharmacological tools to better characterize the role of the MEK5/ERK5 pathway in various biological systems.

纯度：≥98%

CAS：1265916-41-3