Heptelidic Acid

Heptelidic Acid (CAS No.: 57710-57-3) is a fungal-derived sesquiterpene lactone, also known as koningic acid, that exhibits antibiotic and enzyme-inhibitory activities and is widely utilized as a biochemical tool in metabolic and apoptosis research. It functions primarily as an irreversible inhibitor of glyceraldehyde-3-phosphate dehydrogenase (GAPDH) through covalent interaction with the catalytic cysteine residue, thereby suppressing glycolytic ATP production and modulating cellular energy metabolism. In addition, it has been reported to inhibit mammalian DNA polymerases β and λ as well as terminal deoxynucleotidyl transferase, indicating broader effects on DNA repair and replication processes. Heptelidic acid demonstrates biological activity in the low micromolar range and has been shown to modulate apoptotic signaling pathways, including downregulation of caspase activation, resulting in inhibition of etoposide-induced apoptosis, while in highly glycolytic cancer cells it can promote cell death via metabolic stress. Owing to these properties, it is commonly employed in studies investigating glycolysis-dependent cancer cell survival, apoptosis regulation, and enzyme-targeted drug discovery, with experimental concentrations typically optimized according to specific cellular models and assay conditions.