A-769662 | AMPK activator

A-769662 (844499-71-4) is a potent and reversible AMP-activated protein kinase (AMPK) allosteric activator.  Activates AMPK by binding to the β and γ subunits and not the AMP binding site.¹ EC₅₀=0.8 mM for purified rat liver AMPK and inhibits fatty acid biosynthesis in rat hepatocytes IC₅₀=3.2 mM.² A-769662 inhibits the rate of whole-body fatty acid oxidation, decreases body weight gain, reduces plasma and liver triglycerides and lowers plasma glucose in ob/ob mice.² Inhibits adipocyte differentiation.³  Prevents transcriptional activation of Oct4 and establishes a metabolic barrier to induced pluripotent stem cell reprogramming.⁴ A-769662 synergizes with AICAR.⁵ Cell permeable.

References/ A-769662 Citations

1) Scott et al. (2008), Thienopyridone drugs are selective activators of AMP-activated protein kinase beta1-containing complexes; Cell Biol., 15 1220
2) Cool et al. (2006), Identification and characterization of a small molecule AMPK activator that treats key components of type 2 diabetes and the metabolic syndrome; Cell Metab., 3 403
3) Zhou et al. (2009), Inhibitory effects of A-769662, a novel activator of AMP-activated protein kinase on 3T3-L1 adipogenesis; Biol. Pharm. Bull., 32 993
4) Vazquez-Martin et al. (2012) Activation of AMP-activated protein kinase (AMPK) provides a metabolic barrier ro reprogramming somatic cells into stem cells; Cell Cycle, 11 974
5) Ducommun et al. (2014) Enhanced activation of cellular AMPK by dual-small molecule treatment: AICAR and A769662; Am. J. Physiol. Endocrinol. Metab., 306 E688