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Selleckchem/GSK583/S8261

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S8261

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Selleck Chemicals

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DescriptionGSK583 is a highly potent and selective inhibitor of RIP2 kinase with an IC50 of 5 nM.TargetsRIP2 [1](Cell-free assay)RIP3 [1](Cell-free assay)5 nM16 nMIn vitroGSK583 possesses comparable binding affinity for RIP3 kinase as demonstrated by an in-house FP binding assay configured similarly to the RIP2 FP assay (RIP2 FP IC50 = 5 nM; RIP3 FP IC50 = 16 nM). Despite this potent biochemical activity against RIP3 kinase, GSK583 shows little or no inhibition of RIP3-dependent necroptotic cell death in a cellular assay up to 10 μM concentration. GSK583 potently and dose dependently inhibits MDP-stimulated tumor necrosis factor-alpha (TNFα) production with an IC50 = 8 nM in primary human monocytes. Following treatment with GSK583 at 1 μM, little inhibition of pro-inflammatory signaling is observed upon activation of Toll-like receptors (TLR2, TLR4, TLR7) or cytokine receptors (IL-1R, TNFR) but complete inhibition is observed upon activation of both NOD1 and NOD2 receptors, which signal in a RIP2-dependent manner. Although GSK583 has excellent kinase selectivity, it does inhibit both the hERG channel and Cyp3A4, which precludes it from further progression as a drug candidate[1].In vivoGSK583 has low clearance, moderate volumes of distribution, and moderate oral bioavailability in both rat and mouse. Eventhough GSK583 would not produce a human phamacodynamic response within an acceptable dose range which precludes this molecule from further development as a drug candidate, the oral PK in rat and mouse provides sufficient systemic exposure for use as a preclinical in vivo tool molecule in an acute inflammation challenge model[1].

Selleck Chemicals是世界领先的高性能的生命科学产品供应商之一，主要致力于提供MAPK和PI3K/Akt/mTOR等上百个信号通路的高特异性小分子抑制剂。Selleck 产品线补充非常及时，可以提供行业内最新的抑制剂类产品。同时Selleck也是专业的高通量筛选抑制剂分子库、API、天然产物和多肽供应商。