GSK484

GSK484 is a potent, highly selective, and reversible small molecule inhibitor of Peptidyl Arginine Deiminase 4 (PAD4 or PADI4), with a Ki of approximately 50 nM. Developed by GSK as a high-quality chemical probe, it binds to the active site of PAD4 in a calcium-dependent manner, effectively blocking the citrullination of histones (such as Histone H3). This inhibition prevents chromatin decondensation, which is a prerequisite for the formation of Neutrophil Extracellular Traps (NETs). Consequently, GSK484 is widely used in research to investigate the role of NETosis in inflammatory, autoimmune, and malignant diseases. In preclinical models, it has demonstrated efficacy in reducing organ damage in sepsis and limiting the pro-thrombotic and pro-inflammatory effects of NETs.