GKT-137831
NADPH oxidase NOX1/4 inhibitor / 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
Biochemicals & reagents
1218942-37-0
Setanaxib; GKT-831
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
-20°C
TARGET: Nox (NADH/NADPH oxidase); Energy production -- PATHWAY: Redox; NAD, NADP pathways -- RESEARCH AREA: Immunology; Neuroscience -- DISEASE AREA: Cancer; Liver diseaseKidney disease; Atherosclerosis