TAS116 is a selective inhibitor of heat shock protein 90 (Hsp90), specifically targeting the mitochondrial isoform TRAP1 (TNF receptor-associated protein 1). Its primary application lies in cancer research and potential therapeutic development. By inhibiting TRAP1, TAS116 disrupts the protective mechanisms that cancer cells use to survive under stress, leading to the destabilization of oncogenic client proteins and induction of cancer cell death. It has shown particular promise in preclinical studies involving gastrointestinal cancers, including gastric and colorectal cancers, especially those with specific mutations like KRAS or HER2 amplifications. TAS116 enhances the efficacy of other anticancer agents by overcoming resistance mechanisms linked to mitochondrial stress responses. Due to its ability to cross cell membranes effectively and selectively act within mitochondria, TAS116 is used as a tool compound to study mitochondrial protein homeostasis and stress signaling pathways. It is also being explored for its potential in combination therapies, where modulating Hsp90 activity can sensitize tumor cells to chemotherapy, targeted therapy, or immunotherapy.