Disulfiram

别名: NSC 190940, Tetraethylthiuram disulfide, TETD

目录号：S1680 Purity: 99.91%

Disulfiram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。

Disulfiram Chemical Structure

CAS: 97-77-8

规格	价格	库存
10mM (1mL in DMSO)	RMB 490	现货
50mg	RMB 384.93	现货
500mg	RMB 573.99	现货
1g	RMB 959.1	现货
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客户使用Selleck的Disulfiram发表文献36篇

产品质控

批次：纯度： 99.91%

99.91

Disulfiram相关产品

相关靶点	ALDH1A	点击展开
相关化合物库	代谢化合物库抗癌代谢化合物库谷氨酰胺代谢化合物库糖代谢化合物库脂代谢化合物库	点击展开

Dehydrogenase抑制剂选择性比较

细胞实验数据示例

细胞系	实验类型	孵育时间	活性描述	文献信息
MCF7	Antiproliferative assay	72 hrs	Antiproliferative activity against human MCF7 cells expressing BCA2 and estrogen receptor after 72 hrs by MTT assay, IC50 = 0.1 μM.	20222671
CHO	Function assay	30 mins	Inhibition of recombinant human LOXL3 expressed in CHO cells using diaminopentane as substrate preincubated for 30 mins followed by substrate addition measured after 1 hr by fluorimetric method, IC50 = 0.093 μM.	30098867
insect cells	Function assay	30 mins	Inhibition of recombinant human LOXL4 expressed in baculovirus infected insect cells using diaminopentane as substrate preincubated for 30 mins followed by substrate addition measured after 1 hr by fluorimetric method, IC50 = 0.059 μM.	30098867
NS0	Function assay	30 mins	Inhibition of recombinant LOXL2 (unknown origin) expressed in NS0 cells using diaminopentane as substrate preincubated for 30 mins followed by substrate addition measured after 1 hr by fluorimetric method, IC50 = 0.15 μM.	30098867
T47D	Antiproliferative assay	72 hrs	Antiproliferative activity against human T47D cells expressing BCA2 and estrogen receptor after 72 hrs by MTT assay, IC50 = 0.17 μM.	20222671
MDA-MB-231	Antiproliferative assay	72 hrs	Antiproliferative activity against human MDA-MB-231 cells expressing BCA2 and ERalpha after 72 hrs by MTT assay, IC50 = 0.32 μM.	20222671
HEK293	Function assay	30 mins	Inhibition of recombinant human LOX expressed in HEK293 cells using diaminopentane as substrate preincubated for 30 mins followed by substrate addition measured after 1 hr by fluorimetric method, IC50 = 0.32 μM.	30098867
MCF10A	Antiproliferative assay	72 hrs	Antiproliferative activity against human MCF10A cells after 72 hrs by MTT assay, IC50 = 10 μM.	20222671
HepG2	Cytotoxicity assay	72 hrs	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 38 μM.	29571571
CHO	Function assay		Agonist activity at human TRPA1 channel expressed in CHO cells assessed as increase in intracellular calcium levels, EC50 = 3 μM.	20356305
CEM-SS	Antiviral assay		Antiviral activity against HIV-1 in CEM-SS cells using XXT assay, IC50 = 3.9 μM.	9207937
TC32	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
DAOY	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
SJ-GBM2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
A673	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
BT-37	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
NB-EBc1	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
U-2 OS	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
Saos-2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
SK-N-SH	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
NB1643	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
LAN-5	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
BT-12	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
Rh18	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
OHS-50	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
RD	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
MG 63 (6-TG R)	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
fibroblast cells	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells	29435139
Rh41	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
NB1643	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	29435139
A673	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
LAN-5	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	29435139
DAOY	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells	29435139
SJ-GBM2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells	29435139
BT-37	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells	29435139
TC32	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
U-2 OS	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
Rh41	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
RD	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells	29435139
Saos-2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells	29435139
点击查看更多细胞系数据

生物活性

产品描述

靶点

ALDH1 ^[5] (Cell-free assay)	ALDH2 ^[5] (Cell-free assay)
0.15 μM	1.45 μM

体外研究(In Vitro)
体外研究活性	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]

体外研究(In Vitro)

体外研究活性

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]

体内研究(In Vivo)
体内研究活性	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]

体内研究(In Vivo)

体内研究活性

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]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT05626920	Recruiting	Inherited Retinal Dystrophy Primarily Involving Sensory Retina	University of Washington	December 2023	Phase 1\|Phase 2
NCT04485130	Terminated	Covid19	University of California San Francisco	August 18 2021	Phase 2
NCT03151772	Terminated	Glioblastoma	Sahlgrenska University Hospital Sweden	January 29 2018	Early Phase 1
NCT02309801	Completed	Healthy	Parc de Salut Mar\|Ministerio de Sanidad Servicios Sociales e Igualdad	July 2012	Phase 1

参考文献
[1] Chen D, et al. Cancer Res, 2006, 66(21), 10425-10433. [2] Wang W, et al. Int J Cancer, 2003, 104(4), 504-511. [3] Cen D, et al. J Med Chem, 2004, 47(27), 6914-6920. [4] Brar SS, et al. Mol Cancer Ther, 2004, 3(9), 1049-1060. [5] J P Lam, et al. Biochemistry . 1997 Nov 4;36(44):13748-54. [6] Jun Jacob Hu, et al. Nat Immunol . 2020 Jul;21(7):736-745. + 展开

参考文献

+ 展开

化学信息&溶解度

分子量	296.54	分子式	C₁₀H₂₀N₂S₄
CAS号	97-77-8	SDF	Download Disulfiram SDF
Smiles	CCN(CC)C(=S)SSC(=S)N(CC)CC
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : 59 mg/mL ( (198.96 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 59 mg/mL

Water : Insoluble

摩尔浓度计算器

体内溶解度批次：现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂					动物体内配方计算器
体内溶解度批次：现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂	澄清溶液	5%DMSO 1 Corn oil	5mg/ml (16.86mM)	以 1 mL 工作液为例，取50μL100mg/ml的澄清DMSO储备液加到950μL玉米油中，混合均匀。工作液请现配现用！	动物体内配方计算器
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	3.9mg/ml (13.15mM)	以 1 mL 工作液为例,取50μL78mg/ml的澄清DMSO储备液加到400μLPEG300中,混合均匀使其澄清;向上述体系中加入50μLTween80,混合均匀使其澄清;然后继续加入500μLddH2O定容至1mL。工作液请现配现用!
澄清溶液	10%DMSO 1 40%PEG300 2 5%Tween80 3 45%ddH2O	4mg/ml (13.49mM)	以 1 mL 工作液为例，取100μL40mg/ml的澄清DMSO储备液加到400μL PEG300中，混合均匀使其澄清；向上述体系中加入50μLTween80，混合均匀使其澄清；然后继续加入450μL ddH2O定容至 1 mL。工作液请现配现用！

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

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 μL 动物数量只

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

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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