AMP-activated protein kinase (AMPK) plays a role in energy metabolism and glucose homeostasis by monitoring the ratio of ATP to AMP. AMPK stimulates glucose uptake in skeletal muscle when activated during muscle contraction and exercise by the phosphorylation of threonine 172 (Thr172) by LKB19 and Ca2+/calmodulin-dependent kinase kinase. Ampkinone is a small molecule activator of AMPK. It has been shown to stimulate functional activation of AMPK via the phosphorylation at Thr172 in cultured L6 muscle cells with an EC50 value of 4.3 μM, enhancing glucose uptake by 3.2-fold. When given to diet-induced obese mice,10 mg/kg ampkinone up-regulated the activity of AMPK in liver and muscle, enhancing insulin sensitivity and increasing the oxidation of adipose tissues.
