A-769662
AMPK activator / A potent and reversible AMP-activated protein kinase (AMPK) allosteric activator. Activates AMPK by binding to the and subunits and not the AMP binding site1. EC50=0.8 uM for purified rat liver AMPK and inhibits fatty acid biosynthesis in rat hepatocytes IC50=3.2 uM2. 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 mice2. Inhibits adipocyte differentiation3. Prevents transcriptional activation of Oct4 and establishes a metabolic barrier to induced pluripotent stem cell reprogramming4. Synergizes with AICAR5. Cell permeable.
Biochemicals & reagents
844499-71-4
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 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 Cylce, 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
-20°C
TARGET: Kinase -- PATHWAY: Carbohydrate metabolism; Calcium signaling; AMPK pathway -- RESEARCH AREA: Stem cells -- DISEASE AREA: Obesity; Diabetes