GSK484

GSK484 is a highly selective, reversible small-molecule inhibitor of peptidylarginine deiminase 4 (PAD4) with an IC50 of 50 nM in the absence of calcium. Developed by Cellzome (a GSK company) in partnership with the Structural Genomics Consortium (SGC), GSK484 binds to the low-calcium conformation of PAD4, inducing a unique beta-hairpin structure that blocks the enzyme's active site. By inhibiting PAD4, GSK484 prevents the citrullination of histones (such as histone H3), which is a critical step in chromatin decondensation and the subsequent formation of neutrophil extracellular traps (NETs). It is widely utilized as a chemical probe in preclinical research to investigate the role of NETosis and PAD4-mediated citrullination in various inflammatory, autoimmune, and oncological conditions, including rheumatoid arthritis, colitis, deep vein thrombosis, and cancer metastasis.

Other names

GSK 484 HClGSK484 HClGSK-484 HClGSK 484 hydrochlorideGSK484 hydrochlorideGSK-484 hydrochloride