Ampkinone is a small molecule activator of AMPK; stimulate functional activation of AMPK via the phosphorylation at Thr172 in cultured L6 muscle cells with an EC50 value of 4.3 M, enhancing glucose uptake by 3.2-fold.
Ampkinone stimulated the phosphorylation of AMPK via the indirect activation of AMPK in various cell lines. Ampkinone-mediated activation of AMPK required the activity of LKB1 and resulted in increased glucose uptake in muscle cells. In addition, ampkinone-treated DIO mice significantly reduced total body weight and overall fat mass. Histological examination and measurement of lipid parameters showed that ampkinone effectively improved metabolic abnormalities in the DIO mice model.