Protein arginine deiminase 4 (PAD4) mediates the transformation of protein arginine into citrulline. Citrullination of proteins has normal roles in gene regulation and pathological roles in immunological and inflammatory diseases.{18134} GSK484 is a reversible inhibitor of PAD4 (IC50 = 50 nM) that binds to the low-calcium form of the enzyme.{28376} It is selective for PAD4 over PAD1-3. GSK484 blocks the citrullination of PAD4 target proteins in human neutrophils and inhibits the formation of neutrophil extracellular traps in both mouse and human neutrophils.{28376} It exhibits favorable pharmacokinetic profiles in mouse and rat. See the Structural Genomics Consortium (SGC)website for more information.
产品描述
A reversible inhibitor of PAD4 (IC50 = 50 nM) that binds to the low-calcium form of the enzyme; blocks the citrullination of PAD4 target proteins in human neutrophils and inhibits the formation of NETs in both mouse and human neutrophils
