MDH1/2-IN-1 is a MDH1/2 inhibitor (IC50: 1.07 nM and 1.06 nM respectively). MDH1/2-IN-1 inhibits mitochondrial respiration and the HIF-1alpha pathway. MDH1/2-IN-1 demonstrates significant anti-tumor potential. MDH1/2-IN-1 provides a new direction for the development of drugs targeting cancer metabolism[1].