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.
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 vi
vo and leads to increased survival rates in mice bearing highly aggressive human lung tumors. Antitumor agents.
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
