1. Metabolic Enzyme/Protease Immunology/Inflammation Apoptosis
  2. Aldehyde Dehydrogenase (ALDH) Interleukin Related Pyroptosis Apoptosis Cuproptosis
  3. Disulfiram

Disulfiram  (Synonyms: 双硫仑; Tetraethylthiuram disulfide; TETD)

目录号: HY-B0240 纯度: 99.92%
COA 产品使用指南

Disulfiram (Tetraethylthiuram disulfide) 是特异性的乙醛脱氢酶 1 型 (ALDH1) 抑制剂,对酒精具有急性敏感性。Disulfiram 有效抑制人体和小鼠细胞中脂质体中的 GSDMD 孔形成,炎性体介导的细胞凋亡和 IL-1β 分泌。双硫仑 + Cu2+ 可增加细胞内 ROS 水平,引发卵巢癌干细胞凋亡。

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Disulfiram Chemical Structure

Disulfiram Chemical Structure

CAS No. : 97-77-8

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10 mM * 1 mL in DMSO ¥500
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1 g ¥450
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MCE 顾客使用本产品发表的 45 篇科研文献

查看 Aldehyde Dehydrogenase (ALDH) 亚型特异性产品:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Disulfiram (Tetraethylthiuram disulfide) is a specific inhibitor of aldehyde-dehydrogenase (ALDH1), used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells. Disulfiram + Cu2+ increases intracellular ROS levels triggering apoptosis of ovarian cancer stem cells[1-6].

IC50 & Target[1]

IL-1β

 

体外研究
(In Vitro)

在诱导凋亡癌细胞死亡之前,Disulfiram -铜复合物有效抑制培养的乳腺癌 MDA-MB-231 和 MCF10DCIS.com 细胞中的蛋白酶体活性,但不抑制正常的永生化 MCF-10A 细胞[1]。Disulfiram (DS) 是一种临床上使用的抗酒精中毒药物,以剂量依赖性方式强烈抑制本构和 5-FU 诱导的 NF-活化。DisuLfiram 抑制 NF-kappaB 核转位和 DNA 结合活性,但对 5-FU 诱导的 IkappaBalpha 降解没有影响。Disulfiram 显著增强 5-FU 对 DLD-1 和 RKO (WT) 细胞系的凋亡作用,并协同增强 5-FU 对两种细胞系的细胞毒性。DisuLfiram 还在体外有效消除 5-FU 耐药细胞系 H630 (5-FU) 中的 5-FU 化学耐药性[2]。Oseltamivir 降低了活细胞的数量,添加 CuCl2 显著增强了 DSF 诱导的细胞死亡,使其低于对照的 10%[3]。Disulfiram 与 Cu2+ 或 Zn2+ 联合用于黑素瘤细胞可降低细胞周期蛋白 A 的表达,并在低于单独 Disulfiram 的浓度下减少体外增殖[4]
DisuLfiram (0.1 nM-10 μM;72 h) + Cu2+ 组合增强对卵巢癌细胞系的细胞毒性[1]

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

体内研究
(In Vivo)

Disulfiram 显著抑制肿瘤生长(74%),这与携带 MDA-MB-231 肿瘤异种移植物的小鼠体内蛋白酶体抑制和凋亡诱导有关[1]
蛋白酶体抑制是通过肿瘤组织蛋白酶体活性水平降低以及泛素化蛋白和天然蛋白酶体底物 p27 和 Bax[1] 的积累来衡量的。
细胞凋亡表现为 caspase 激活和凋亡细胞核形成[1]
Disulfiram 阻断 P-糖蛋白挤出泵,抑制转录因子核因子-kappaB,使肿瘤对化疗敏感,减少血管生成,抑制小鼠肿瘤生长[4]
Disulfiram 抑制移植到严重联合免疫缺陷小鼠体内的黑色素瘤的生长和血管生成,这些作用通过补充 Zn2+ 得到加强[4]

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

Clinical Trial
分子量

296.54

Formula

C10H20N2S4

CAS 号
性状

固体

颜色

White to yellow

中文名称

双硫仑;二硫龙;二硫化四乙基秋兰姆

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 1 year
-20°C 6 months
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 75 mg/mL (252.92 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.3722 mL 16.8611 mL 33.7223 mL
5 mM 0.6744 mL 3.3722 mL 6.7445 mL
查看完整储备液配制表

* 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°C, 1 years; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

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

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (7.01 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

    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;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (7.01 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

    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 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。

以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 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。

  • 方案 一

    请依序添加每种溶剂: Corn Oil

    Solubility: 30 mg/mL (101.17 mM); 澄清溶液; 超声助溶

  • 方案 二

    请依序添加每种溶剂: 50% PEG300    50% Saline

    Solubility: 10 mg/mL (33.72 mM); 悬浊液; 超声助溶

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.92%

参考文献
Cell Assay
[4]

The effect of disulfiram (0.15-5.0 μM) or sodium diethyldithiocarbamate (1.0 μM) on proliferation of malignant cell lines is studied in cultures stimulated with 10% FBS. Cell numbers are quantitated 24 to 72 hours later, as outlined below. In some experiments, disulfiram is added immediately after cells are plated. In other experiments, cells are plated and allowed to grow for 24 to 72 hours before fresh medium with disulfiram is added and cell numbers are assayed 24 to 72 hours later. Synergy is studied between disulfiram and N,N′-bis(2-chloroethyl-N-nitrosourea (carmustine, 1.0-1,000 μM) or cisplatin (0.1-100 μg/mL) added to medium. The effect of metal ions on disulfiram is studied with 0.2 to 10 μM Cu2+ (provided as CuSO4), Zn2+ (as ZnCl2), Ag+ (as silver lactate), or Au3+ (as HAuCl4·3H2O) ions added to growth medium, buffered to physiologic pH. To provide a biologically relevant source of copper, medium is supplemented with human ceruloplasmin at doses replicating low and high normal adult serum concentrations (250 and 500 mg/mL).

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

Animal Administration
[4]

Adult female CB17-SCID mice are housed in a protected laminar flow facility with access to water and either a standard diet containing 87 ppm zinc or a zinc-supplemented diet containing 1,000 ppm Zn2+ as zinc acetate. Mice are injected s.c. in the right groin with 5×106 cells from a highly aggressive malignant melanoma obtained from a Carolinas Medical Center patient. The frozen tumor is passaged twice in SCID mice to adapt it to in vivo growth before use in these experiments. On the day of tumor injection, all mice began daily administration of drug. Drug is given in a total volume of 0.2 mL by gastric gavage via smooth Teflon-tipped needles inserted transorally into the stomach. Four groups are studied: tumor control (n=10; 0.2 mL olive oil daily; zinc diet of 87 ppm); zinc-supplemented control (n=10; 0.2 mL olive oil daily; zinc diet of 1,000 ppm); disulfiram (n=10; 200 mg/kg/d disulfiram in 0.2 mL olive oil; zinc diet of 87 ppm); and zinc-supplemented diet + disulfiram (n=10; 200 mg/kg/d disulfiram in 0.2 mL olive oil; zinc diet of 1,000 ppm). Mice are examined daily, the tumor is measured in two dimensions, and the tumor volume is estimated using the formula for an elipse. When estimated tumor volume approached 500 mm3 within any animal, all mice are euthanized. Tumors are excised, weighed, fixed in formalin, sectioned, and stained or immunostained for factor VIII. Slides are coded and examined by a blinded observer who identified vessels as deposits of red cells. For each slide, the number of vessels is counted in four different fields representative of the tumor. The average number of vessels per field is averaged per biopsy specimen and used to evaluate tumor vascularity.

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

参考文献

完整储备液配制表

* 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°C, 1 years; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3722 mL 16.8611 mL 33.7223 mL 84.3057 mL
5 mM 0.6744 mL 3.3722 mL 6.7445 mL 16.8611 mL
10 mM 0.3372 mL 1.6861 mL 3.3722 mL 8.4306 mL
15 mM 0.2248 mL 1.1241 mL 2.2482 mL 5.6204 mL
20 mM 0.1686 mL 0.8431 mL 1.6861 mL 4.2153 mL
25 mM 0.1349 mL 0.6744 mL 1.3489 mL 3.3722 mL
30 mM 0.1124 mL 0.5620 mL 1.1241 mL 2.8102 mL
40 mM 0.0843 mL 0.4215 mL 0.8431 mL 2.1076 mL
50 mM 0.0674 mL 0.3372 mL 0.6744 mL 1.6861 mL
60 mM 0.0562 mL 0.2810 mL 0.5620 mL 1.4051 mL
80 mM 0.0422 mL 0.2108 mL 0.4215 mL 1.0538 mL
100 mM 0.0337 mL 0.1686 mL 0.3372 mL 0.8431 mL
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HY-B0240
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