GNF351

GNF351 is a potent and selective small molecule antagonist of the Aryl-hydrocarbon receptor (AhR). The AhR is a ligand-activated transcription factor that regulates the expression of genes involved in xenobiotic metabolism and immune response. In the context of oncology, AhR activation in the tumor microenvironment can lead to immunosuppression and tumor growth. GNF351 is frequently used as a pharmacological tool to study AhR biology and has demonstrated synergistic cytotoxic effects when combined with proteasome pathway inhibitors, such as bortezomib and TAK-243, in various patient-derived cancer models including glioblastoma and pancreatic cancer. It was originally developed by the Genomics Institute of the Novartis Research Foundation (GNF).

Other names

N-(2-(1H-indol-3-yl)ethyl)-9-isopropyl-2-(5-methylpyridin-3-yl)-9H-purin-6-amine