GSK583 (1346547-00-9) is a highly selective and potent inhibitor of RIP2 kinase, IC50?= 5 nM human and IC50?= 2 nM rat.1?It also potently inhibits isolated RIP3 kinase (IC50?= 5 nM) but is inactive against RIP3 in cellular assays due to a very low KM,ATP. GSK583 blocks NOD2 signaling by interfering with XIAP-RIP2 binding resulting in decreased cytokine and chemokine production.1,2
GSK 583, is a selective inhibitor of RIP-like interacting CLARP kinase RIP2 Kinase is a central component of the innate immune system and enables downstream signaling following activation of the pattern recognition receptors NOD1 and NOD2, leading to the production of inflammatory cytokines.
1) Haile?et al.?(2016),?The Identification and Pharmacological Characterization of 6-(tert-Butylsulfonyl)-N-(5-fluoro-1H-indazol-3-yl)quinoline-4-amine; J. Med. Chem.,?59?4867
2) Goncharov?et al.?(2018),?Disruption of XIAP-RIP2 Association Blocks NOD2-Mediated Inflammatory Signaling; Mol. Cell,?69?551
