Disulfiram
别名: NSC 190940, Tetraethylthiuram disulfide, TETD 中文名称：
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
产品质控
批次：
纯度：
99.91%
99.91
Disulfiram相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 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 | 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。 | ||||
|---|---|---|---|---|---|
| 靶点 |
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| 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] |
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|---|---|---|---|---|
| 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] |
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|---|---|---|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| 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 |
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) | |||
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体外溶解度 |
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 (198.96 mM) Water : Insoluble |
摩尔浓度计算器 |
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体内溶解度 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 | ||||
实验计算
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）
mg/kg
g
μL
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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