Dimethyl fumarate (DMF) 是一种具有口服活性且可透过血脑屏障的Nrf2激活剂,可诱导抗氧化剂基因表达上调。Dimethyl fumarate 通过 GSH 耗竭/ROS升高/MAPKs 激活途径诱导结肠癌细胞坏死,并诱导细胞自噬 (autophagy)。Dimethyl fumarate 可用于多发性硬化症的研究。
生物活性 | Dimethyl fumarate (DMF) is an orally active and brain-penetrantNrf2activator and induces upregulation of antioxidant gene expression. Dimethyl fumarate inducesnecroptosisin coloncancercells through GSH depletion/ROSincrease/MAPKs activation pathway, and also induces cellautophagy. Dimethyl fumarate can be used for multiple sclerosis research[1][2]. |
IC50& Target | Human Endogenous Metabolite |
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体外研究 (In Vitro) | Dimethyl fumarate (DMF; 20-200 μM; 24 hours) treatment dose-dependently reduces the viability of SGC-7901, HT29, HCT116 and CT26 cancer cells[1]. Dimethyl fumarate (DMF; 100 μM; 3-24 hours) significantly activates JNK, p38 and ERK in CT26 cells[1]. Dimethyl fumarate induces necroptosis in colon cancer cells and the mechanism involves GSH depletion, an increase in ROS and activation of MAPKs-mediated signalling[1]. Dimethyl fumarate inhibits dendritic cell (DC) maturation by reducing inflammatory cytokine production (IL-12 and IL-6) and the expression of MHC class II, CD80, and CD86. Dimethyl fumarate impairs NF-κB signaling via reduced p65 nuclear translocalization and phosphorylation. Dimethyl fumarate inhibits maturation of DCs and subsequently Th1 and Th17 cell differentiation by suppression of both NF-κB and ERK1/2-MSK1 signaling[2]. Dimethyl fumarate (DMF), an immune modulator and inducer of the antioxidant response, suppresses HIV replication and neurotoxin release[3].
Cell Viability Assay[1] Cell Line: | SGC-7901, HT29, HCT116 and CT26 cells | Concentration: | 20 μM, 50 μM, 100 μM, 200 μM | Incubation Time: | 24 hours | Result: | Reduced cell viability in SGC-7901, HT29, HCT116 and CT26 cancer cells. |
Western Blot Analysis[1] Cell Line: | CT26 cancer cells | Concentration: | 100 μM | Incubation Time: | 3 hours, 6 hours, 12 hours, 24 hours | Result: | Significantly activated JNK, p38 and ERK in CT26 cells after treatment from 3 to 24 h. |
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体内研究 (In Vivo) | Dimethyl fumarate (DMF; 50 mg/kg; oral gavage; daily; for 7 days) treatment is shown to upregulate the mRNA and protein levels of Nrf2 and Nrf2-regulated cytoprotective genes, attenuate 6-OHDA induced striatal oxidative stress and inflammation in C57BL/6 mice[4].
Animal Model: | Male C57BL/6 mice (8-week-old)[4] | Dosage: | 50 mg/kg | Administration: | Oral gavage; daily; for 7 days | Result: | Was shown to upregulate mRNA and protein levels of Nrf2 and Nrf2-regulated cytoprotective genes. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 50 mg/mL(346.91 mM;Need ultrasonic) H2O : 8.33 mg/mL(57.80 mM;ultrasonic and warming and heat to 60℃) 配制储备液 1 mM | 6.9382 mL | 34.6909 mL | 69.3818 mL | 5 mM | 1.3876 mL | 6.9382 mL | 13.8764 mL | 10 mM | 0.6938 mL | 3.4691 mL | 6.9382 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 50%PEG300 50% saline Solubility: 7.5 mg/mL (52.04 mM); Suspended solution; Need ultrasonic 2. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (14.43 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (14.43 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 3. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (14.43 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (14.43 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 4. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (14.43 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (14.43 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 5. 请依序添加每种溶剂: PBS Solubility: 2 mg/mL (13.88 mM); Clear solution; Need ultrasonic and warming and heat to 60℃ *以上所有助溶剂都可在本网站选购。
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