Potent and selective ERK5 inhibitor; inhibits EGFR-induced ERK5 autophosphorylation (EC50
= 90 nM) and ERK5 enzymatic activity (IC50
= 162 nM). Exhibits at least 30-fold selectivity for ERK5 over LRRK2 in a cell based assay. Also selective for ERK5 over a panel of other kinases. Orally bioavailable.
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All Tocris products are intended for laboratory research use only.
Sold under license from Dana-Farber Cancer Institute.
Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones.
Deng et al.
X-ray crystal structure of ERK5 (MAPK7) in complex with a specific inhibitor.
Elkins et al.