Cas No.: | 1346547-00-9 |
Chemical Name: | 6‑(tert-Butylsulfonyl)‑N‑(5-fluoro‑1H‑indazol-3-yl)quinolin-4-amine |
Synonyms: | GSK583,GSK-583,GSK 583 |
SMILES: | FC1=CC2=C(NN=C2NC3=CC=NC4=CC=C(S(=O)(C(C)(C)C)=O)C=C34)C=C1 |
Formula: | C20H19FN4O2S |
M.Wt: | 398.12 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | GSK583 is a highly potent and selective inhibitor of RIP2 Kinase, with IC50 of 5 nM. |
In Vivo: | GSK583 (0.1, 1, and 10 mg/kg, p.o.) inhibits serum KC (the rodent orthologue of IL-8) levels in rats in a dose-dependent manner, with an IC50 derived from rat blood concentrations of 50 nM (or 20 ng/mL). Similarly, GSK583 inhibits serum KC levels and recruitment of neutrophils into the peritoneal cavity in mice in a dose-dependent manner, with an IC50 of 37 nM (15 ng/mL) derived from mouse blood concentration[1]. |
In Vitro: | GSK583 (1 μM) exhibits excellent selectivity in a panel of 300 kinases, including p38α and VEGFR2. GSK583 potently and dose dependently inhibits MDP-stimulated tumor necrosis factor-alpha (TNFα) production with an IC50 of 8 nM. GSK583 demonstrates only a modest reduction in potency when profiled in a similar MDP-induced TNFα production assay in human whole blood (IC50 = 237 nM) and rat whole blood (IC50 = 133 nM)[1]. |