GKT-137831 | NADPH oxidase NOX1/4 inhibitor

GKT-137831 (1218942-37-0) is an NADPH oxidase, NOX1/4 inhibitor (K_i = 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