GSK583

GSK583 is a highly potent, selective, and cell-permeable small molecule inhibitor of receptor-interacting serine/threonine-protein kinase 2 (RIPK2, also known as RIP2 kinase). Developed by GSK, it acts as an ATP-competitive inhibitor with nanomolar potency. RIPK2 is a key mediator of the innate immune system, transducing signals downstream of the pattern recognition receptors NOD1 and NOD2 to drive the production of pro-inflammatory cytokines. Although GSK583 demonstrated strong efficacy in blocking NOD1- and NOD2-mediated inflammatory responses in cellular, rodent in vivo, and human ex vivo disease models (such as Crohn's disease and ulcerative colitis), its development as a clinical drug candidate was discontinued due to off-target activity against the hERG ion channel and a suboptimal pharmacokinetic profile. It is widely utilized as a preclinical research tool.

Other names

6-((1,1-dimethylethyl)sulfonyl)-N-(5-fluoro-1H-indazol-3-yl)-4-quinolinamine6-(tert-butylsulfonyl)-N-(5-fluoro-1H-indazol-3-yl)quinolin-4-amine