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Product Details

GKT-137831 | NADPH oxidase NOX1/4 inhibitor

GKT-137831 (1218942-37-0) is an NADPH oxidase, NOX1/4 inhibitor (Ki = 100-150 nM).1  Inhibits erastin-stimulated ROS production.2 Potentiates immunotherapy by overcoming cancer-associated fibroblast- mediated CD8+ T-cell exclusion.3 Reduces ROS production in LPS-stimulated platelets in a mouse model.4 Reduces subarachnoid hemorrhage-induced neuronal death.5 Potent inhibitor of experimental liver fibrosis in mouse models.6

References/Citations
1) Jiang et al. (2012), Liver fibrosis and hepatocyte apoptosis are attenuated by GKT137831, a novel NOX4/NOX1 inhibitor in vivo; Free Radic. Biol. Med., 53 289
2) Dachert et al. (2020), Targeting ferroptosis in rhabdomyosarcoma cells; Int. J. Cancer, 146(2) 510
3) Ford et al. (2020), NOX4 Inhibition Potentiates Immunotherapy by Overcoming Cancer-Associated Fibroblast-Mediated CD8 T-cell Exclusion from Tumors; Cancer Res., 80 1846
4) Naime et al. (2019), Tumor necrosis factor alpha has a crucial role in increased reactive oxygen species production in platelets of mice injected with lipopolysaccharide; Platelets, 30 1047
5) Zhang et al. (2017), Involvement of Nox2 and Nox4 NADPH oxidases in early brain injury after subarachnoid hemorrhage; Free Radic. Res., 51 316
6) Aoyama et al. (2012), Nicotinamide adenine dinucleotide phosphate oxidase in experimental liver fibrosis: GKT137831 as a novel potential therapeutic agent; Hepatology, 56 2316

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Catalog#  10-5044-0005

$70.00
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Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
1218942-37-0
Catalog Number:
10-5044
Activity:
NADPH oxidase NOX1/4 inhibitor
Chemical Name:
2-(2-Chlorophenyl)-4-[3-(dimethylamino)phenyl]-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
Alternate Name:
Setanaxib
Molecular Weight:
394.85
Molecular Formula:
C21H19ClN4O2
Solubility:
Soluble in DMSO (up to 65 mg/ml).
Physical Properties:
Pale yellow solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 2 years as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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