GSK2795039

GSK2795039 is a selective, small-molecule inhibitor of NADPH oxidase 2 (NOX2), an enzyme complex that generates reactive oxygen species (ROS) in immune cells such as neutrophils, macrophages, and microglia. Discovered by GSK, the compound acts by competing with NADPH at its binding site on NOX2, thereby blocking superoxide/ROS production and NADPH consumption. It exhibits high selectivity for NOX2 over other NOX isoforms (NOX1, NOX3, NOX4, and NOX5), as well as xanthine oxidase and endothelial nitric oxide synthase (eNOS). GSK2795039 has been widely utilized as a preclinical research tool to investigate the role of NOX2-derived oxidative stress in various animal models, including acute pancreatitis, traumatic brain injury, neuropathic pain, and inflammation. However, due to its short half-life and limited selectivity, it has not progressed to clinical development, serving instead as a reference compound and a starting point for the design of optimized analogs.

Other names

N-(1-Isopropyl-3-(1-methylindolin-6-yl)-1H-pyrrolo[2,3-b]pyridin-4-yl)-1-methyl-1H-pyrazole-3-sulfonamideN-[3-(2,3-Dihydro-1-methyl-1H-indol-6-yl)-1-(1-methylethyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-1-methyl-1H-pyrazole-3-sulfonamide