中文名：GSK2795039
英文名：GSK2795039
纯度：≥99%
货号：G414304
Cas号：1415925-18-6
存储温度：-20°C储存
运输条件：超低温运输
产品介绍：
Information
GSK2795039 GSK2795039 is an inhibitor of NADPH oxidase 2 (NOX2) with pIC50 of 6.57 for NOX2-mediated activation of HRP/Amplex Red. GSK2795039 inhibits reactive oxygen species (ROS) production, NADPH consumption and reduces apoptosis .
Targets
ROS ; NADPH ; NOX2 (HRP/Amplex Red) (Cell-based assay) ; 6.57(pIC50)
In vitro
GSK2795039 inhibits both the formation of ROS and the utilization of the enzyme substrates, NADPH and oxygen, in a variety of semirecombinant cell-free and cell-based NOX2 assays. GSK2795039 inhibits NOX2 in an NADPH competitive manner and is selective over other NOX isoforms, xanthine oxidase, and endothelial nitric oxide synthase enzymes.
In vivo
Following systemic administration in mice, GSK2795039 abolishes the production of ROS by activated NOX2 enzyme in a paw inflammation model. GSK2795039 shows activity in a murine model of acute pancreatitis, reducing the levels of serum amylase triggered by systemic injection of cerulein.
Cell Research(from reference)
Cell lines：NOX isoform-specific cells, PBMCs, PMNs, HL60 cells
Concentrations：3.16 nM, 10 nM, 31.6 nM, 100 nM, 316 nM, 1μM, 3.16 μM, 10 μM, 31.6 μM, 100μM
Incubation Time：10 min, 20 min, 30 min, 40 min, 50 min, 60 min
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关键字： 1H-?Pyrazole-?3-?sulfonamide,N-?[3-?(2,?3-?dihydro-?1-?methyl-?1H-?indol-?6-?yl)?-?1-?(1-?methylethyl)?-?1H-?pyrrolo[2,?3-?b]?pyridin-?4-?yl]?-?1-?methyl-
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