AGB-374 is an orally active NDUFS7 inhibitor. It destabilizes the NDUFS7 protein and inhibits oxidative phosphorylation by targeting mitochondrial complex I. In vivo, AGB-374 reduces MYC protein levels in colon cancer cells and slows tumor growth in homologous mouse models of colon cancer. AGB-374 synergistically enhances the cytotoxicity of copper chelators against cancer cells and downregulates MYC and NDUFS7 protein levels in these cells when used in combination with copper chelators. AGB-374 is useful for colon cancer research.