Elesclomol-Cu

Elesclomol-Cu(II), is a cell-permeable, complex of potent copper ionophore Elesclomol with copper II (Cu2+) that selectively targets the mitochondria of cancer cells reliant on oxidative phosphorylation (OXPHOS). Its core action involves ferredoxin 1 (FDX1)-mediated reduction within the mitochondrial matrix, releasing toxic Cu(I) to initiate a dual cell death cascade. This comprises both overwhelming oxidative stress leading to apoptosis and cuproptosis, a distinct, genetically-defined mechanism driven by the aggregation of lipoylated TCA cycle proteins, whose core components (such as FDX1 and DLAT) serve as key biomarkers. This unique FDX1-dependent process confers nanomolar cytotoxicity and synergistic in vivo efficacy, making it an invaluable probe for dissecting the interplay between metal homeostasis, mitochondrial metabolism, and proteotoxic stress.