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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GSK2795039
Dangerous GoodsCAS number：1415925-18-6 molecular formula：C23H26N6O2S
overview
compound introduction
Specs
| Chinese alias | - | ||
| English alias | 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- | ||
| CAS number | 1415925-18-6 | molecular formula | C23H26N6O2S |
| molecular weight | 450.56 g/mol | Exact mass | 10mM in DMSO |
| PSA | 93.400 Ų | logp | 3.536 |
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physicochemical properties
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Safety information
pictogram：
GHS07
Signal word：
Warning
Hazard Statement：
H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激
Statement of Preventive Measures：
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。
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