IM-156 is an inhibitor of mitochondrial complex I, also known as NADH dehydrogenase (IC50 = 2.2 µM) and an activator of AMP-activated protein kinase α (AMPKα). It reduces the oxygen consumption rate (OCR; IC50 = 3.3 µM) and decreases mitochondrial ATP production in Eµ-Myc mouse lymphoma cells. IM-156 (10, 30, and 50 µM) increases AMPKα activity in primary rat peritoneal mesothelial cells and protects against chlorhexidine-induced peritoneal fibrosis in rats when administered at a dose of 1 mg/kg. It reduces tumor growth in an AT-84 murine oral cancer model and decreases age-related decline in novel object recognition, spatial working, and contextual memory in mice.