6,2',4'-Trimethoxyflavone - CAS 720675-74-1
Category: Inhibitor
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Aryl Hydrocarbon Receptors
6,2',4'-Trimethoxyflavone is an aryl hydrocarbon receptor antagonist (EC50 = 0.9 μM), displaying no short term agonist activity and no species or promoter dependence.
Brife Description:
aryl hydrocarbon receptor antagonist
≥97% by HPLC
2',4',6-Trimethoxyflavone; 2-(2,4-dimethoxyphenyl)-6-methoxy-4H-chromen-4-one
Canonical SMILES:
1.Kynurenine Modulates MMP-1 and Type-I Collagen Expression Via Aryl Hydrocarbon Receptor Activation in Dermal Fibroblasts.
Poormasjedi-Meibod MS;Salimi Elizei S;Leung V;Baradar Jalili R;Ko F;Ghahary A J Cell Physiol. 2016 Dec;231(12):2749-60. doi: 10.1002/jcp.25383. Epub 2016 Apr 4.
Dermal fibrosis is characterized by a high deposition of extracellular matrix (ECM) and tissue cellularity. Unfortunately all means of treating this condition are unsatisfactory. We have previously reported the anti-fibrotic effects of Kynurenine (Kyn), a tryptophan metabolite, in fibrotic rabbit ear model. Here, we report the mechanism by which Kyn modulates the expression of key ECM components in dermal fibroblasts. The results showed that Kyn activates aryl hydrocarbon receptor (AHR) nuclear translocation and up-regulates cytochrome-P450 (CYP1A-1) expression, the AHR target gene. A specific AHR antagonist, 6,2',4'-trimethoxyflavone, inhibited the Kyn-dependent modulation of CYP1A-1, MMP-1, and type-I collagen expression. Establishing the anti-fibrogenic effect of Kyn and its mechanism of action, we then developed nano-fibrous Kyn slow-releasing dressings and examined their anti-fibrotic efficacy in vitro and in a rat model. Our results showed the feasibility of incorporating Kyn into PVA/PLGA nanofibers, prolonging the Kyn release up to 4 days tested. Application of medicated-dressings significantly improved the dermal fibrosis indicated by MMP-1 induction, alpha-smooth muscle actin and type-I collagen suppression, and reduced tissue cellularity, T-cells and myofibroblasts.
2.Ah receptor antagonism represses head and neck tumor cell aggressive phenotype.
DiNatale BC;Smith K;John K;Krishnegowda G;Amin SG;Perdew GH Mol Cancer Res. 2012 Oct;10(10):1369-79. doi: 10.1158/1541-7786.MCR-12-0216. Epub 2012 Aug 21.
The aryl hydrocarbon receptor (AhR) has been shown to play a role in an increasing number of cellular processes. Recent reports have linked the AhR to cell proliferation, cytoskeletal arrangement, and tumor invasiveness in various tumor cell types. The AhR plays a role in the de-repression of the interleukin (IL)6 promoter in certain tumor cell lines, allowing for increased transcriptional activation by cytokines. Here, we show that there is a significant level of constitutive activation of the AhR in cells isolated from patients with head and neck squamous cell carcinoma (HNSCC). Constitutive activation of the AhR in HNSCCs was blocked by antagonist treatment, leading to a reduction in IL6 expression. In addition, the AhR exhibits a high level of expression in HNSCCs than in normal keratinocytes. These findings led to the hypothesis that the basal AhR activity in HNSCCs plays a role in the aggressive phenotype of these tumors and that antagonist treatment could mitigate this phenotype. This study provides evidence that antagonism of the AhR in HNSCC tumor cells, in the absence of exogenous receptor ligands, has a significant effect on tumor cell phenotype. Treatment of these cell lines with the AhR antagonists 6, 2', 4'-trimethoxyflavone, or the more potent GNF351, decreased migration and invasion of HNSCC cells and prevented benzo[a]pyrene-mediated induction of the chemotherapy efflux protein ABCG2.
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CAS 720675-74-1 6,2',4'-Trimethoxyflavone

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