NCIt definition : An orally bioavailable inhibitor of the nicotinamide adenine dinucleotide phosphate
(NADPH) oxidases (NOX) 1 and 4, with potential anti-inflammatory, anti-fibrotic and
antineoplastic activities. Upon oral administration, setanaxib targets, binds to and
inhibits the activity of NOX1 and NOX4. This inhibits NOX1- and NOX4- mediated signal
transduction pathways, thereby reducing inflammation and fibrosis. By targeting NOX4-overexpressing
cancer-associated fibroblasts (CAFs) in the tumor microenvironment (TME), setanaxib
may also inhibit myofibroblastic activation and enhance both the penetration of tumor-infiltrating
lymphocytes (TILs) and antitumor T-cell immune responses. The NOX enzymes NOX1 and
NOX4 primarily produce reactive oxygen species (ROS), which plays important roles
in cellular signaling processes that regulate cell proliferation, differentiation
and migration, and inflammation and fibrosis.;
UNII : 45II35329V;
InChIKey : RGYQPQARIQKJKH-UHFFFAOYSA-N;
CAS number : 1218942-37-0;
Molecule name : GKT-831; GKT 831; GKT-137831; GKT 137831;