2. Immunology/Inflammation Metabolic Enzyme/Protease Apoptosis PI3K/Akt/mTOR Stem Cell/Wnt MAPK/ERK Pathway TGF-beta/Smad
  3. Aryl Hydrocarbon Receptor Cytochrome P450 Apoptosis Akt ERK TGF-beta/Smad
  4. 3'-Methoxy-4'-nitroflavone

3'-Methoxy-4'-nitroflavone (MNF) 是一种特异性的芳烃受体 (AhR) 拮抗剂。3'-Methoxy-4'-nitroflavone 通过抑制内源性配体 FICZ (HY-12451) 的代谢酶 (CYP1)，导致 FICZ 累积，从而激活 AhR。3'-Methoxy-4'-nitroflavone 逆转 TCDD 的抗凋亡 (apoptosis) 作用，减弱 TCDD 对 Akt 和 Erk1/2 激酶的激活和 TGFα 表达。3'-Methoxy-4'-nitroflavone 可用于乳腺肿瘤促进、类风湿性关节炎、多发性硬化症和炎症性肠病的相关研究。

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3'-Methoxy-4'-nitroflavone

3'-Methoxy-4'-nitroflavone Chemical Structure

CAS No. : 145370-39-4

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3'-Methoxy-4'-nitroflavone 相关抗体

Top Publications Citing Use of Products

查看 Cytochrome P450 亚型特异性产品:

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

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ERK ERK1 ERK2 ERK5 ERK8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

3'-Methoxy-4'-nitroflavone (MNF) is a specific aryl hydrocarbon receptor (AhR) antagonist. 3'-Methoxy-4'-nitroflavone activates AhR by inhibiting CYP1, the metabolic enzyme of the endogenous ligand FICZ (HY-12451), leading to the accumulation of FICZ. 3'-Methoxy-4'-nitroflavone reverses the anti-apoptotic effect of TCDD, attenuates the activation of Akt and Erk1/2 kinases and the expression of TGFα induced by TCDD. 3'-Methoxy-4'-nitroflavone can be used in research related to breast tumor promotion, rheumatoid arthritis, multiple sclerosis and inflammatory bowel disease[1][2].

体外研究
(In Vitro)

3'-Methoxy-4'-nitroflavone (0.1-1000 nM; 24 h) 可在低至 10 nM 的浓度下抑制 MCF-10A 细胞中 TCDD 依赖性 DRE 驱动的荧光素酶活性[1]。
3'-Methoxy-4'-nitroflavone (0.1-1000 nM; 3 days) 可逆转 TCDD 对 MCF-10A 细胞凋亡的依赖性抑制作用，在 100 nM 和 1000 nM 浓度下可观察到显著效应[1]。
3'-Methoxy-4'-nitroflavone (0.1-1000 nM; 6 h) 可减弱 MCF-10A 细胞中 Akt 的磷酸化水平，在 1 nM 时可观察到显著抑制作用，在 100 nM 时则可实现完全抑制[1]。
3'-Methoxy-4'-nitroflavone (0.1-1000 nM; 6 h) 可在 10 nM 及以上浓度下逆转 MCF-10A 细胞中 TCDD 介导的 Erk1,2 磷酸化，且在单独作用时，其 1 nM 浓度可增强基础 Erk1,2 的激活[1]。
3'-Methoxy-4'-nitroflavone (0.1-100 nM; 6 h) 可在低至 1 nM 的浓度下完全消除 MCF-10A 细胞中 TCDD 依赖性的 TGFα mRNA 表达[1]。
3'-Methoxy-4'-nitroflavone (0.5-2.5 μM) 可强效抑制人重组 CYP1A1 的基础乙氧基试卤灵脱乙基酶活性[2]。
3'-Methoxy-4'-nitroflavone (0.05-2.5 μM; 1.5-20 h) 可在体外以剂量依赖的方式抑制 2,3,7,8-四氯二苯并-对-二恶英诱导的 HaCaT 细胞中乙氧基试卤灵脱乙基酶活性[2]。
3'-Methoxy-4'-nitroflavone (0.05-2.5 μM; 1.5-48 h) 在 HaCaT 细胞中先抑制后增强 FICZ 依赖的 CYP1A1 mRNA 表达以及乙氧基试卤灵脱乙基酶活性，在延长孵育时间下可观察到显著的增强效应[2]。
3'-Methoxy-4'-nitroflavone (0.05-2.5 μM; 0-40 h) 可在 HaCaT 细胞中诱导依赖于芳香烃受体的乙氧基试卤灵脱乙基酶活性，该作用依赖于培养基中的内源性 FICZ[2]。
3'-Methoxy-4'-nitroflavone (0.05 μM; 0-30 h) 可在 HaCaT 细胞中诱导依赖于芳香烃受体的 CYP1A1 mRNA 表达，该过程需要商用细胞培养基中存在的 FICZ[2]。
3'-Methoxy-4'-nitroflavone (50 nM; 48 h) 仅在存在 0.1 pM FICZ 的情况下，可诱导 HaCaT 细胞中的乙氧基试卤灵脱乙基酶活性[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

3'-Methoxy-4'-nitroflavone 相关抗体:

Apoptosis Analysis[1]

Cell Line: MCF-10A human mammary epithelial cells
Concentration: 0.1 nM, 1 nM, 10 nM, 100 nM, 1000 nM (co-treated with 10 nM TCDD)
Incubation Time: 3 days
Result: Resulted in four times the number of apoptotic cells compared to TCDD alone at 100 nM.
Doubled the number of apoptotic cells compared to TCDD alone at 1000 nM.

Western Blot Analysis[1]

Cell Line: MCF-10A human mammary epithelial cells
Concentration: 0.1 nM, 1 nM, 10 nM, 100 nM, 1000 nM (co-treated with 10 nM TCDD); 0.1 nM, 1 nM, 10 nM, 100 nM, 1000 nM (treated alone)
Incubation Time: 6 h
Result: Decreased TCDD-induced Akt serine phosphorylation at 1 nM.
Induced complete inhibition of TCDD-induced Akt serine phosphorylation at 100 nM.
Caused a slight increase in TCDD-induced Akt phosphorylation at 10 nM.
Had minimal effect on basal Akt phosphorylation when treated alone.\nInhibited TCDD-dependent Erk1,2 phosphorylation at 10 nM, 100 nM, and 1000 nM.
Significantly increased basal Erk1,2 activation alone at 1 nM.

Real Time qPCR[1]

Cell Line: MCF-10A human mammary epithelial cells
Concentration: 0.1 nM, 1 nM, 10 nM, 100 nM (co-treated with 10 nM TCDD); 0.1 nM, 1 nM, 10 nM, 100 nM (treated alone)
Incubation Time: 6 h
Result: Completely reversed the TCDD-induced 2-fold increase in TGFα mRNA at concentrations as low as 1 nM.
Increased TGFα mRNA over basal levels alone at 0.1 nM.

Real Time qPCR[2]

Cell Line: HaCaT cells
Concentration: 0.05 μM
Incubation Time: 0, 10, 20 and 30 h
Result: Significantly induced CYP1A1 mRNA expression in cells cultured in commercial DMEM, with no significant induction observed in cells cultured in DMEM with recrystallized tryptophan.
分子量

297.26

Formula

C16H11NO5
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

3'-Methoxy-4'-nitroflavone 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

3'-Methoxy-4'-nitroflavone145370-39-4MNFAryl Hydrocarbon ReceptorCytochrome P450ApoptosisAktERKTGF-beta/SmadAhRCYPsPKBProtein kinase BExtracellular signal regulated kinasesTransforming growth factor betadioxin response elementHaCaT cellsTCDDMCF-10A cellsaryl hydrocarbon receptorErk1,2TGFαFICZcytochrome P450 1A1Inhibitorinhibitorinhibit

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