Size | Price | Stock |
---|---|---|
2mg | $84 | In-stock |
5mg | $168 | In-stock |
10mg | $264 | In-stock |
50mg | $900 | In-stock |
100mg | $1440 | In-stock |
200 mg | Get quote | |
500 mg | Get quote | |
We match the lowest price on market. |
We offer a substantial discount on larger orders, please inquire via [email protected]
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Cat. No. : | HY-100339 |
M.Wt: | 398.45 |
Formula: | C20H19FN4O2S |
Purity: | >98 % |
Solubility: | DMSO : ≥ 100 mg/mL (250.97 mM) |
GSK583 is a highly potent, orally active and selective inhibitor of RIP2 Kinase, with IC50 of 5 nM. GSK583 inhibits both TNF-α and IL-6 production with an IC50 value of 200 nM. IC50 & Target: IC50: 5 nM (RIP2K)[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]. 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].
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