GPX4 allosteric activator

A GPX4 allosteric activator is a class of small molecule compounds designed to bind to an allosteric site on glutathione peroxidase 4 (GPX4), thereby enhancing its enzymatic activity. GPX4 is a selenium-dependent antioxidant enzyme that plays a critical role in protecting cells from lipid peroxidation by reducing phospholipid hydroperoxides to their corresponding alcohols. By activating GPX4, these compounds inhibit ferroptosis—an iron-dependent form of regulated cell death—and suppress associated inflammatory pathways, such as the NF-κB pathway. GPX4 allosteric activators, such as PKUMDL-LC-101-D04 (compound 102) and GPX4 activator 1, are being investigated in preclinical research for their potential therapeutic applications in lipid-peroxidation-mediated and ferroptosis-driven conditions, including heart failure with preserved ejection fraction (HFpEF), spinal cord injury, and neurodegenerative diseases.

Other names

GPX4 activatorGPX-4 activatorGPX 4 activatorglutathione peroxidase 4 activatorglutathione peroxidase 4 allosteric activator