Biochem/physiol Actions
BAY-885 is an ATP site-targeting, potent and selective ERK5 (BMK1, MAPK7) inhibitor (IC50 = 35 nM with 250 µM ATP; % inhibition at 1 µM = 62/rat Fer, 58/human EphB3, 43/human EphA5, =20/355 kinases) with no BRD4 affinity (20 µM), nor inhibitory potency toward hERG (10 µM) and CYP enzymes (20 µM; CYP1A2, CYP2C8, CYP2C9, CYP2D6, CYP3A4). BAY-885 potently inhibits 100 ng/mL EGF-induced, ERK5-dependent MEF2 activity (IC50 = 120 nM; SN12C-MEF2-luc reporter assay).
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