1346547-00-9

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.

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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