MK-2206

A highly selective non-ATP competitive allosteric Akt inhibitor with IC₅₀’s of 8 nM, 2 nM and 65 nM for Akt1, Akt2 and Akt3, respectively. MK-2206 potently inhibits phosphorylation of Thr³⁰⁸ and Ser⁴⁷³ in 3T3-L1 adipocytes with IC₅₀ values of 0.11 and 0.18 µM, respectively as well as downstream effects of insulin on GLUT4 translocation (IC₅₀ = 0.47 µM) and glucose transport (IC₅₀ = 0.14 µM). In addition, treatment with MK-2206 causes a robust, concentration-dependent activation of autophagy in human glioma cell lines LN229 and T98G.