GSK583
RIP2 kinase inhibitor / GSK583 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 RPI3 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
Biochemicals & reagents
1346547-00-9
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
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TARGET: Kinase -- PATHWAY: Cytokine; TNF -- RESEARCH AREA: Immunology -- DISEASE AREA: Infectious disease; Inflammation