MK-2206 (CAS 1032350-13-2) is a potent and selective allosteric inhibitor of Akt (IC50’s: Akt1 = 5 nM, Akt2 = 12 nM, Akt3 = 65 nM) that enhances the?in vitro?and?in vivo?antitumor efficacy of several standard chemotherapeutic agents.1?It was able to decrease insulin-stimulated glucose uptake, glycogen synthesis and glycogen synthase activity in rat muscle.2?MK-2206 induced G1-phase cycle arrest and sensitized HepG2 hepatocellular carcinoma cells to TRAIL-induced apoptosis.3
AZD 6244 and MK 2206 are targeted small-molecule drugs that inhibit MEK and AKT responses. The combination of AZD6244 and MK2206 has a significant synergistic effect on tumor growth in vitro and in vivo and leads to increased survival rates in mice bearing highly aggressive human lung tumors. Antitumor agents. Potent AKT inhibitor.
A highly selective inhibitor of Akt. Akt1, IC50=8 nM; Akt2, IC50=12 nM; Akt3, IC50=65 nM.
1) Hirai?et al.?(2010),?MK-2206, an Allosteric Akt inhibitor, Enhances Antitumor Efficacy by Standard Chemotherapeutic Agents or Molecular targeted Drugs In vitro and In vivo; Mol. Cancer Ther.?9?1956
2) Lai?et al.?(2012),?A novel PKB/Akt inhibitor, MK-2206, effectively inhibits insulin-stimulated glucose metabolism and protein synthesis in isolated rat skeletal muscle; Biochem. J.?447?137
3) Jiao?et al.?(2013),?MK-2206 induces cell cycle arrest and apoptosis in HepG2 cells and sensitizes TRAIL-mediated cell death; Mol. Cell Biochem.?382?217
