2-Trifluoromethyl-2'-methoxychalcone

Nrf2 activation is central to cytoprotective gene expression against oxidative and/or electrophilic stress.{17702} Unless activated by inflammatory, environmental, or oxidative stressors, Nrf2 is sequestered in the cytoplasm by its repressor, Keap1.{16386} Because of its protective capabilities, small molecules that activate Nrf2 signaling are being examined as potential anti-cancer or anti-inflammatory agents.{20661} 2-Trifluoromethyl-2'-methoxychalcone is a potent activator of Nrf2, both in vitro and in mice.{21374} Human bronchial epithelial cells treated with 10 ?M 2-trifluoromethyl-2'-methoxychalcone showed a marked increase in the expression of the Nrf2-regulated antioxidant genes, GCLM and NQO1. Furthermore, treatment of mice with 50 mg/kg 2-trifluoromethyl-2’-methoxychalcone leads to a 4.5- and 4.6-fold increase in the expression of GCLM and NQO1, respectively, in the small intestine.{21374}