Synonyms: GSK583; 6-(tert-Butylsulfonyl)-N-(5-fluoro-1H-indazol-3-yl)quinolin-4-amine; GSK'583; GSK-2616583A
Molecular Formula: C20H19FN4O2S
Molecular Weight: 398.45
Linear Structural Formula: C20H19FN4O2S
Purity: >=98% (HPLC)
Storage: 2-8C
Biochem Physiol Actions: GSK583 is a cell-permeable indazolylquinolinamine that acts as an ATP-competitive (IC50 = 2 & 5 nM using rat & human RIPK2, respectively) inhibitor against RIPK2 kinase activity (66.6% inhibition at 1 muM; [ATP] = 10 muM), exhibiting much reduced or no inhibitory potency against a panel of 209 other kinases <34 % inhibition at 1 mum; [atp]="10" m). gsk583 selectively inhibits against nod1- and nod2-, but not tlr2-, tlr4-, tlr7-. il-1r-, or tnfr-dependent pro-inflammatory cytokines release (>95% inhibition vs.<40 % inhibition at 1 m using primary human monocytes stimulated with respective ligands). gsk583 effectively inhibits tnf? and il-6 production from crohn s disease (cd) and ulcerative colitis (uc) patients intestinal explant cultures ex vivo (ic50="200" nm) and is efficacious against nod1 ligand fk156- and nod2 ligand mdp-induced inflammatory responses in mice and rats (10 mg g p.o.) in vivo.<>