Erk5-In-1, Potent And Selective Erk5 Inhibitor, Each

Details:

Erk5-in-1 is a 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.