Dimethyl 2-ketoglutarate is an esterified form of the citric acid cycle intermediate α-ketoglutarate. It increases intracellular levels of α-ketoglutarate and decreases intracellular ATP levels in U2OS human osteosarcoma cells cultured in complete- or nutrient-free media when used at a concentration of 5 mM. Dimethyl 2-ketoglutarate inhibits autophagy and decreases in intracellular levels of acetyl-CoA in serum- and nutrient-deprived cells. It decreases cardiomyocyte hypertrophy in a mouse model of cardiac pressure overload induced by thoracic aortic constriction when administered at a dose of 300 mg/kg. Dimethyl 2-ketoglutarate reduces serum levels of aspartate aminotransferase (AST) and alanine aminotransferase (ALT) and hepatic fibrosis in a rat model of liver fibrosis induced by carbon tetrachloride (CCl4).