GSK2982772

GSK2982772 is a first-in-class, orally active small molecule that acts as a highly selective inhibitor of receptor-interacting protein kinase 1 (RIPK1). RIPK1 is a serine-threonine kinase involved in the regulation of TNF-mediated apoptosis and necroptosis as well as inflammatory pathways. By binding to an allosteric pocket of the RIPK1 kinase domain, GSK2982772 inhibits RIPK1-mediated cell death and cytokine production. The drug has been developed primarily for chronic inflammatory diseases such as ulcerative colitis and rheumatoid arthritis. Clinical studies have demonstrated its safety and tolerability at doses up to 120 mg twice daily in healthy volunteers[6][4][3].

Other names

(S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-1H-1,2,4-triazole-3-carboxamide1622848-92-3