GSK2795039

GSK2795039 is an inhibitor of NADPH oxidase 2 (NOX2; IC50 = 0.269 µM). It is selective for NOX2 over NOX1, -3, -4, and -5 (IC50s = >1,000 µM for all), as well as xanthine oxidase and PKCβ (IC50s = 28.8 and 10 µM, respectively). GSK2795039 inhibits NOX2-mediated production of reactive oxygen species (ROS) and NADPH depletion in cell-free assays (IC50s = 0.537 and 0.251 µM, respectively). In vivo, GSK2795039 (100 mg/kg) reduces serum levels of amylase, a marker for pancreatic cell necrosis, in a gp91phox knockout mouse model of acute pancreatitis. GSK2795039 also inhibits brain NOX2 activity, decreases...