MK-2206 | Potent and selective AKT inhibitor

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

References/Citations

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