XMD8-85 is a selective ERK5 inhibitor with IC50 of 87 nM in enzyme assay.
XMD8-85 is selective for ERK5 over tyrosine non-receptor kinase 2 (TNK2, IC50=959 nM), but does inhibit the leucine-rich repeat kinase 2 (LRRK2) mutant LRRK2G2019S (IC50 = 26 nM).
XMD8-85 inhibits EGF-induced ERK5 autophosphorylation in HeLa cells (EC50= 0.19 μM).
XMD8-85 also inhibits Brd4/BET family bromodomains, transcriptional regulators required for Nanog expression.
