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Disulfiram Sale

(Synonyms: 双硫仑; Tetraethylthiuram disulfide; TETD) 目录号 : GC10801

An irreversible inhibitor of aldehyde dehydrogenase

Disulfiram Chemical Structure

Cas No.:97-77-8

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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Kinase experiment [1]:

Binding assays

The chymotrypsin-like activity of purified 20S proteasome was measured. Briefly, 17.5 ng of purified 20S proteasome were incubated in 100 μL of assay buffer (50 mmol/L Tris-HCl, pH 7.5) with or without different concentrations of copper chloride, Disulfiram, or the Disulfiram-copper mixture and 10 μmol/L fluorogenic peptide substrate Suc-LLVY-AMC (for the proteasomal chymotrypsin-like activity) for 2 hrs at 37℃. After incubation, production of hydrolyzed AMC groups was measured with a Wallac Victor3 multilabel counter with an excitation filter of 365 nm and an emission filter of 460 nm.

Cell experiment [1]:

Cell lines

MDA-MB-231 cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

5 ~ 20 μM; 24 hrs

Applications

The Disulfiram-copper complex potently inhibited the proteasomal activity in cultured breast cancer MDA-MB-231 cells, before induction of apoptotic cancer cell death.

Animal experiment [1]:

Animal models

Mice bearing MDA-MB-231 tumor xenografts

Dosage form

50 mg/kg/d; p.o.; 29 days

Applications

In mice bearing MDA-MB-231 tumor xenografts, Disulfiram significantly inhibited tumor growth (by 74%), associated with in vivo proteasome inhibition and apoptosis induction.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Chen D, Cui QC, Yang H, Dou QP. Disulfiram, a clinically used anti-alcoholism drug and copper-binding agent, induces apoptotic cell death in breast cancer cultures and xenografts via inhibition of the proteasome activity. Cancer Res. 2006 Nov 1;66(21):10425-33.

产品描述

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[1-4].

Disulfiram-copper complex potently inhibits the proteasomal activity in cultured breast cancer MDA-MB-231 and MCF10DCIS.com cells, but not normal, immortalized MCF-10A cells, before induction of apoptotic cancer cell death[1]. Disulfiram (DS), a clinically used anti-alcoholism drug, strongly inhibits constitutive and 5-FU-induced NF-kappaB activity in a dose-dependent manner. Disulfiram inhibits both NF-kappaB nuclear translocation and DNA binding activity but has no effect on 5-FU-induced IkappaBalpha degradation. Disulfiram significantly enhances the apoptotic effect of 5-FU on DLD-1 and RKO(WT) cell lines and synergistically potentiated the cytotoxicity of 5-FU to both cell lines. Disulfiram also effectively abolishes 5-FU chemoresistance in a 5-FU resistant cell line H630(5-FU) in vitro[2]. Oseltamivir decreases the number of viable cells, and the addition of CuCl2 significantly enhances the DSF-induced cell death to less than 10% of control[3]. Disulfiram given to melanoma cells in combination with Cu2+ or Zn2+ decreases expression of cyclin A and reduces proliferation in vitro at lower concentrations than disulfiram alone[4].

Disulfiram significantly inhibits the tumor growth (by 74%), associated with in vivo proteasome inhibition (as measured by decreased levels of tumor tissue proteasome activity and accumulation of ubiquitinated proteins and natural proteasome substrates p27 and Bax) and apoptosis induction (as shown by caspase activation and apoptotic nuclei formation) in mice bearing MDA-MB-231 tumor xenografts[1]. Disulfiram blocks the P-glycoprotein extrusion pump, inhibits the transcription factor nuclear factor-kappaB, sensitizes tumors to chemotherapy, reduces angiogenesis, and inhibits tumor growth in mice. Disulfiram inhibits growth and angiogenesis in melanomas transplanted in severe combined immunodeficient mice, and these effects are potentiated by Zn2+ supplementation[4].

References:
[1]. Chen D, ert al. Disulfiram, a clinically used anti-alcoholism drug and copper-binding agent, induces apoptotic cell death in breast cancer cultures and xenografts via inhibition of the proteasome activity. Cancer Res. 2006 Nov 1;66(21):10425-33.
[2]. Wang W, et al. Disulfiram-mediated inhibition of NF-kappaB activity enhances cytotoxicity of 5-fluorouracil in human colorectal cancer cell lines. Int J Cancer. 2003 Apr 20;104(4):504-11.
[3]. Cen D, et al. Disulfiram facilitates intracellular Cu uptake and induces apoptosis in human melanoma cells. J Med Chem. 2004 Dec 30;47(27):6914-20.
[4]. Brar SS, et al. Disulfiram inhibits activating transcription factor/cyclic AMP-responsive element binding protein and human melanoma growth in a metal-dependent manner in vitro, in mice and in a patient with metastatic disease. Mol Cancer Ther. 2004 Sep;3
[5]. Jun Jacob Hu, et al. Identification of pyroptosis inhibitors that target a reactive cysteine in gasdermin D. The Preprint Server For Biology, 2018,Jul. 10.

Chemical Properties

Cas No. 97-77-8 SDF
别名 双硫仑; Tetraethylthiuram disulfide; TETD
化学名 diethylcarbamothioylsulfanyl N,N-diethylcarbamodithioate
Canonical SMILES CCN(CC)C(=S)SSC(=S)N(CC)CC
分子式 C10H20N2S4 分子量 296.54
溶解度 ≥ 12 mg/mL in DMSO, ≥ 24.2 mg/mL in EtOH with ultrasonic 储存条件 Store at 4°C
General tips 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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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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
10 mM 0.3372 mL 1.6861 mL 3.3722 mL
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