6,2',4'-Trimethoxyflavone

6,2',4'-Trimethoxyflavone is a potent aryl hydrocarbon receptor (AHR) antagonist. 6,2',4'-Trimethoxyflavone represses AHR-mediated gene induction^[1]. In Vitro: 6,2',4'-trimethoxyflavone (TMF) as an AHR ligand that possesses the characteristics of an antagonist having the capacity to compete with agonists, such as 2,3,7,8-tetrachlorodibenzo-p-dioxin and benzo[a]pyrene, thus effectively inhibiting AHR-mediated transactivation of a heterologous reporter and endogenous targets, e.g., CYP1A1, independent of cell lineage or species. Furthermore, TMF displays superior action by virtue of having no partial agonist activity, in contrast to other documented antagonists, e.g., alpha-napthoflavone, which are partial weak agonists. TMF also exhibits no species or promoter dependence with regard to AHR antagonism^[1].
6,2',4'-Trimethoxyflavone (0-100 μM; 72 hours) shows an inhibitory activity of TNF- production in THP-1 cells, with IC₅₀ of 2.38 μM. 6,2',4'-Trimethoxyflavone shows an inhibitory activity of TNF-α production in B16-F10 cells with IC₅₀ of 1.32 μM^[2]. In Vivo: 6,2',4'-trimethoxyflavone-treated (5 mg/kg/day; i.p.) WT mice shows significantly decreased infarct volume, improved sensorimotor, and nonspatial working memory functions compared with their respective controls^[3].