Description: Trametinib (GSK1120212) is a MEK inhibitor that inhibits MEK1 and MEK2 (IC50=0.7/0.9 nM) with ATP non-competitive and oral activity. Trametinib activates autophagy and induces apoptosis. Target: Apoptosis, MEK, Autophagy. Smiles:...

GSK1120212 inhibits MEK1/2 and is currently in clinical trials as a potential treatment for melanoma. GSK1120212 exhibits anticancer chemotherapeutic activity, upregulating p27 expression and inhibiting growth in colorectal cancer cells and suppressing tumor growth in colorectal cancer xenografts.

Trametinib is an inhibitor of MEK1 and -2. It inhibits B-RAF- and C-RAF-induced phosphorylation of MEK1 (IC50s = 3.4 and 1.8 nM, respectively) and MEK2 (IC50s = 1.6 and 0.92 nM, respectively). Trametinib inhibits the growth of two human colorectal cancer cell lines expressing mutant B-RAF (IC50s = 0.48 and 0.52 nM)...

Soluble in DMSO. Slightly soluble (<1mg/ml) in ethanol. GSK1120212 (JTP-74057, trametinib) is a highly specific and potent MEK1 and MEK2 inhibitor with IC(50) values of 0.92nM and 1.8nM respectively. Target: MEK1 - MEK2 , Kinase Group: STE , Substrate: Serine-Threonine