1218942-37-0

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

2-(2-Chlorophenyl)-4-(3-(dimethylamino)phenyl)-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione is a potential drug candidate, which is used in the preparation of pyrazolopyridine derivative as NADPH oxidase inhibitors.

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