Trametinib (GSK1120212): Selectivity & Specificity
Trametinib (GSK1120212) is a potent inhibitor of MEK1 (4.75 nM), BRaf-MEK1 (0.001 nM), MEK2 (14.40 nM), BRaf-MEK2 (0.465 nM), and MEK (<250 nM). Trametinib (GSK1120212) exhibits the greatest inhibitory potency toward BRaf-MEK1 (IC50 = 0.001 nM).