Disulfiram (NSC 190940)

For research use only. Not for use in humans.

目录号:S1680 别名: Tetraethylthiuram disulfide, TETD

Disulfiram (NSC 190940) Chemical Structure

CAS No. 97-77-8

Disulfiram (NSC 190940, Tetraethylthiuram disulfide, TETD)是一个特异性的乙醛脱氢酶 aldehyde-dehydrogenase (ALDH) 抑制剂,对hALDH1和hALDH2的IC50值分别0.15 μM和1.45 μM。Disulfiram 可用于治疗慢性酒精中毒,对酒精产生急性敏感性。Disulfiram 可诱导凋亡。Disulfiram 还是一种通过 gasdermin D (GSDMD) 作用的孔隙形成抑制剂。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1063.76 现货
RMB 814.86 现货
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客户使用Selleck生产的Disulfiram (NSC 190940)发表文献23篇:

产品安全说明书

Dehydrogenase抑制剂选择性比较

生物活性

产品描述 Disulfiram (NSC 190940, Tetraethylthiuram disulfide, TETD)是一个特异性的乙醛脱氢酶 aldehyde-dehydrogenase (ALDH) 抑制剂,对hALDH1和hALDH2的IC50值分别0.15 μM和1.45 μM。Disulfiram 可用于治疗慢性酒精中毒,对酒精产生急性敏感性。Disulfiram 可诱导凋亡。Disulfiram 还是一种通过 gasdermin D (GSDMD) 作用的孔隙形成抑制剂。
靶点
ALDH1 [5]
(Cell-free assay)
ALDH2 [5]
(Cell-free assay)
0.15 μM 1.45 μM
体外研究

在乳腺癌细胞MDA-MB-231和MCF10DCIS.com细胞中,Disulfiram铜配合物诱在导凋亡的癌细胞死亡前有效抑制培养的蛋白酶体的活性,而不在正常的,永生化的MCF-10A细胞中发挥这样的作用。[1] Disulfiram,在临床上使用的抗酒精中毒的药物,以剂量依赖性的方式强烈抑制组成和5-FU诱导的NF-κB活性。Disulfiram既抑制NF-κB的核转位和DNA结合活性,但对5-FU诱导的IkappaBalpha降解没有影响。在DLD-1和RKO(WT)细胞系中,Disulfiram显著增强5-FU的凋亡作用并协同增强5-FU的细胞毒性。在5-FU的耐药细胞系H630中,Disulfiram也有效地废除5-FU化疗效果。[2] Disulfiram降低活细胞的数量,加入氯化铜显著增强DSF诱导的细胞死亡,比对照组低10%。[3] 在黑素瘤细胞中,与较低浓度Disulfiram相比,Disulfiram与铜离子和锌离子联用可降低细胞周期蛋白A的表达,并减少在体外增殖。[4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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MG 63 (6-TG R) MWHxTHRUKGG|c3H5 MUfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN? MoDHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
fibroblast cells NF7KdHpyUFSVIHHzd4F6 MoP2dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKGOxboTyc4whUGhid3ns[EB1gXCnIH\pZpJw[myjc4SgZ4VtdHN? M1vOWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh41 NWTKWXhkeUiWUzDhd5NigQ>? M13Y[ZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCUaESxJINmdGy| NFnNcWM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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LAN-5 NV7ETIpZeUiWUzDhd5NigQ>? MmmydWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgUGFPNTViY3XscJM> NG\1PIc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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SJ-GBM2 NEfwUlByUFSVIHHzd4F6 M3L3PZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNLNUeETUKgZ4VtdHN? M3fQbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
BT-37 M3e5WpFJXFNiYYPzZZk> MY\xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDCWE0{PyClZXzsdy=> Mm\vQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
TC32 NEm1b2RyUFSVIHHzd4F6 MULxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDUR|MzKGOnbHzz NEnFenY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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Rh41 NWjhb4dreUiWUzDhd5NigQ>? MWXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDSbFQyKGOnbHzz NUnFRXZHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
RD MUDxTHRUKGG|c3H5 M1HwUJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHJFKGOnbHzz NE\zfII9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Saos-2 MX;xTHRUKGG|c3H5 NU\mOol1eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW2Gxcz2yJINmdGy| MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-

... Click to View More Cell Line Experimental Data

体内研究

Disulfiram显著抑制肿瘤生长达74%,这和体内蛋白酶抑制相关联(通过减少的水平的肿瘤组织蛋白酶活性和泛素化的蛋白质和天然蛋白酶底物的p27和Bax的积累的测量)。Disulfiram还诱导细胞凋亡(通过半胱天冬荷瘤小鼠的MDA-MB-231肿瘤异种移植物的活化和凋亡细胞核的形成)。[1] Disulfiram阻断P-糖蛋白挤压泵,抑制转录因子核因子-κB,使肿瘤对化疗敏感,减少血管生成,并抑制小鼠肿瘤的生长。在黑色素瘤移植的严重联合免疫缺陷小鼠中,Disulfiram抑制生长和血管生成,这些效果是通过锌离子补充加强。[4]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

溶解度 (25°C)

体外 DMSO 59 mg/mL (198.96 mM)
Water Insoluble
Ethanol ''''''59 mg/mL
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
2.5mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 296.54
化学式

C10H20N2S4

CAS号 97-77-8
储存条件 粉状
溶于溶剂
别名 Tetraethylthiuram disulfide, TETD

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04485130 Recruiting Drug: Disulfiram|Drug: Placebo Covid19 University of California San Francisco May 1 2021 Phase 2
NCT03151772 Terminated Drug: Disulfiram|Drug: Metformin Glioblastoma Sahlgrenska University Hospital Sweden January 29 2018 Early Phase 1
NCT02309801 Completed Dietary Supplement: Daidzin|Dietary Supplement: Alcohol Healthy Parc de Salut Mar|Ministerio de Sanidad Servicios Sociales e Igualdad July 2012 Phase 1
NCT01286259 Completed Drug: Disulfiram HIV-1 Infection University of California San Francisco|Johns Hopkins University January 2011 Not Applicable
NCT02101008 Completed Drug: disulfiram and chelated zinc Melanoma University of Utah March 2010 Phase 2

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项
免费分装抑制剂

Dehydrogenase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID