货号 | 11881-100mg |
描述 | Nrf2 activation is central to cytoprotective gene expression against oxidative and/or electrophilic stress.1 Unless activated by inflammatory, environmental, or oxidative stressors, Nrf2 is sequestered in the cytoplasm by its repressor, Keap1.2 Because of its protective capabilities, small molecules that activate Nrf2 signaling are being examined as potential anti-cancer or anti-inflammatory agents.3 2-Trifluoromethyl-2-methoxychalcone is a potent activator of Nrf2, both in vitro and in mice.4 Human bronchial epithelial cells treated with 10 μM 2-trifluoromethyl-2-methoxychalcone showed a marked increase in the expression of the Nrf2-regulated antioxidant genes, GCLM and NQO1. Furthermore, treatment of mice 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 compared to controls.4 |
供应商 | Cayman |
应用文献 | |
1.Wang, R.,Kern, J.T.,Goodfriend, T.L., et al. Activation of the antioxidant response element by specific oxidized metabolites of linoleic acid. Prostaglandins, Leukotrienes and Essential Fatty Acids 81, 53-59 (2009). 2.Gao, L.,Wang, J.,Sekhar, K.R., et al. Novel n-3 fatty acid oxidation products activate Nrf2 by destabilizing the association between Keap1 and Cullin3. The Journal of Biological Chemisty 282(4), 2529-2537 (2007). 3.Taguchi, K.,Motohashi, H., and Yamamoto, M. Molecular mechanisms of the Keap1-Nrf2 pathway in stress response and cancer evolution. Genes to Cells 16, 123-140 (2011). 4.Kumar, V.,Kumar, S.,Hassan, M., et al. Novel chalcone derivatives as potent Nrf2 activators in mice and human lung epithelial cells. Journal of Medicinal Chemistry 54(12), 4147-4159 (2011). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 306.3 |
分子式 | C17H13F3O2 |
CAS号 | 1309371-03-6 |
稳定性 | ≥ 1 year |
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