Disulfiram 是一种特异性的乙醛脱氢酶 1 型抗体抑制剂，对酒精具有急性敏感性。它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。

Disulfiram is a carbamate derivative used as an alcohol deterrent. It is a relatively nontoxic substance when administered alone, but markedly alters the intermediary metabolism of alcohol. When alcohol is ingested after administration of disulfiram, blood acetaldehyde concentrations are increased, followed by flushing, systemic vasodilation, respiratory difficulties, nausea, hypotension, and other symptoms (acetaldehyde syndrome). It acts by inhibiting aldehyde dehydrogenase.

Disulfiram阻断P-糖蛋白挤压泵,抑制转录因子核因子-κB,降低血管生成,并抑制小鼠肿瘤的生长.Disulfiram抑制肿瘤作用和体内蛋白酶抑制相关联.Disulfiram还诱导细胞凋亡.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,锌离子可以补充加强这种效果.

Disulfiram在临床上作为抗酒精中毒的药物,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。DLD-1和RKO（WT）细胞系中,Disulfiram可以明显增强5-FU的凋亡作用并协同增强5-FU的细胞毒性。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减少细胞周期蛋白A的表达,并抑制在体外的增殖。 Disulfiram降低活细胞的数量,加入氯化铜明显增强DSF诱导的细胞死亡。

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 HAuCl4·3Water) 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).

97-77-8

C10H20N2S4

296.52

TETD;双硫仑;双硫伦;Tetraethylthiuram disulfide;NSC 190940

Ethanol:29.7 mg/mL (100 mM)
DMSO:29.7 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years