IACS-010759 is a potent and selective Oxidative Phosphorylation Inhibitor (IC₅₀ < 10 nM) with potential antineoplastic activity. IACS-010759 robustly inhibits proliferation and induces apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS, likely owing to a combination of energy depletion and reduced aspartate production that leads to impaired nucleotide biosynthesis.