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.
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.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay
Cell Line: |
THP-1 cells, B16-F10 cells |
Concentration: |
0-100 μM |
Incubation Time: |
72 hours |
Result: |
Showed inhibitory activity of TNF-? production in THP-1 cells and B16-F10 cells.
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