BAY-439

BAY-439 is a potent, selective, small-molecule inhibitor of human phospholipase A2 group V (hPLA2-G5, encoded by the PLA2G5 gene) with single-digit nanomolar activity. Developed by Bayer in collaboration with Evotec, BAY-439 was identified through high-throughput and fragment-based screening and subsequently optimized for its physicochemical and pharmacokinetic properties. It acts as an active-site inhibitor of hPLA2-G5, which is elevated in inflammatory conditions and plays a key role in neutrophil and macrophage recruitment, arachidonic acid release, and PGE2 production. BAY-439 has been accepted as a donated chemical probe by the Structural Genomics Consortium (SGC) to facilitate open-science research into the physiological and pathological roles of hPLA2-G5, particularly in inflammatory pain conditions such as endometriosis.

Other names

BAY 439BAY439BAY-439