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MEK inhibitor is an inhibitor of MEK5 (IC50 = 1.5 nM).1 It is selective for MEK5 over ERK5, activin receptor-like kinase 5 (ALK5), also known as TGF-β receptor type I (TGF-βRI), MEK1, and MEK2 (IC50s = 59, 580, >6,300, and >6,300 nM, respectively) and a panel of 79 other kinases at 10 µM. MEK inhibitor (1, 3, or 10 µM) decreases the levels of phosphorylated ERK5 in sorbitol-stimulated HeLa cells. It inhibits TGF-β1-induced increases in N-cadherin levels, decreases in E-cadherin levels, and cell migration in a scratch assay in A549 lung cancer cells when used at a concentration of 10 µM.2 MEK inhibitor (20 mg/kg per day) decreases the number of lung nodules in an A549 mouse model of lung metastasis.
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1. BIX02189 inhibits TGF-