GSK583 | RIP2 kinase inhibitor

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 K_M,ATP. GSK583 blocks NOD2 signaling by interfering with XIAP-RIP2 binding resulting in decreased cytokine and chemokine production.^1,2

References/Citations
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