Disulfiram (Synonyms: Tetraethylthiuram disulfide; TETD)

Name: Disulfiram
Brand: MedChemExpress
SKU: HY-B0240
Rating: 5.0 (92 reviews)

Cat. No.: HY-B0240 Purity: 99.78%: FAQs
Data Sheet
SDS

COA
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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. Disulfiram, a copper ion carrier, with Cu²⁺ increases intracellular ROS levels and induces cuproptosis.

For research use only. We do not sell to patients.

Disulfiram Chemical Structure

CAS No. : 97-77-8

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
100 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	In-stock	Estimated Time of Arrival: December 31
1 g	In-stock	Estimated Time of Arrival: December 31
5 g	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 92 publication(s) in Google Scholar

Other Forms of Disulfiram:

Disulfiram (Standard) Get quote

87 Publications Citing Use of MCE Disulfiram

Cell Viability Assay

Angiogenesis Assay

MMP Analysis

IHC

: Disulfiram purchased from MedChemExpress. Usage Cited in: Bioact Mater. 2024 Mar 1:36:96-111. [Abstract]; Disulfiram (DSF) (0.5 μM; 12 h); CuCy (0.5 μM; 12 h). Mitochondrial membrane potential assay and DAPI staining.

: Disulfiram purchased from MedChemExpress. Usage Cited in: Bioact Mater. 2024 Mar 1:36:96-111. [Abstract]; Disulfiram (DSF) (0.5 μM; 3-5 h). Vessel formation assay of HUVEC cells after drug treatment.

: Disulfiram purchased from MedChemExpress. Usage Cited in: Bioact Mater. 2024 Mar 1:36:96-111. [Abstract]; Disulfiram (DSF) (0.5 μM; 12-24 h). Protein levels of Caspase-9, Caspase-3, Cleaved Caspase-9, and Cleaved Caspase-3 were evaluated by Western blotting after 12 and 24 h of drug treatment

: Disulfiram purchased from MedChemExpress. Usage Cited in: Bioact Mater. 2024 Mar 1:36:96-111. [Abstract]; Disulfiram (DSF) (0.5 μM; local injection; once every 3 days, 5 times in total); CuCy (0.5 μM; local injection; once every 3 days, 5 times in total). Results of H&E staining for subcutaneously transplanted tumors and organs (heart, liver, spleen, lung, kidney) in mice. Additionally, TUNEL staining results for the transplanted tumors.

: Disulfiram purchased from MedChemExpress. Usage Cited in: Bioact Mater. 2024 Mar 1:36:96-111. [Abstract]; (b) Cytotoxic effects of different concentrations CuCl2, CuCy, and Disulfiram (DSF) (12.5-200 μM) and (c) Combination therapy with different concentrations of CuCy (0.5 μM; 24 h) and DSF (0.5 μM; 24 h) on Ishikawa cells.

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View All Aldehyde Dehydrogenase (ALDH) Isoform Specific Products:

View All Isoforms

ALDH1 ALDH2 ALDH3

View All Interleukin Related Isoform Specific Products:

View All Isoforms

IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

IL-1β

Cellular Effect

Cell Line	Type	Value	Description	References
4T1	IC₅₀	0.25 μM Compound: 29; DSF	Anticancer activity against mouse 4T1 cells assessed as cell growth inhibition by MTS assay Anticancer activity against mouse 4T1 cells assessed as cell growth inhibition by MTS assay	[PMID: 33650861]
CEM-SS	IC₅₀	> 100 μM Compound: disulfiram	Antiviral activity against HIV-1ADA in CEM-SS cells using monocyte/macrophage cultures Antiviral activity against HIV-1ADA in CEM-SS cells using monocyte/macrophage cultures	[PMID: 9207937]
CEM-SS	IC₅₀	3.9 μM Compound: disulfiram	Antiviral activity against HIV-1 in CEM-SS cells using XXT assay Antiviral activity against HIV-1 in CEM-SS cells using XXT assay	[PMID: 9207937]
HepG2	IC₅₀	38 μM Compound: Disulfiram	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 29571571]
MCF-10A	IC₅₀	10 μM Compound: 1, DSF	Antiproliferative activity against human MCF10A cells after 72 hrs by MTT assay Antiproliferative activity against human MCF10A cells after 72 hrs by MTT assay	[PMID: 20222671]
MCF7	IC₅₀	0.1 μM Compound: 1, DSF	Antiproliferative activity against human MCF7 cells expressing BCA2 and estrogen receptor after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells expressing BCA2 and estrogen receptor after 72 hrs by MTT assay	[PMID: 20222671]
MDA-MB-231	IC₅₀	> 10 μM Compound: 1, DSF	Antiproliferative activity against BCA2 and ER deficient human MDA-MB-231 cells after 72 hrs by MTT assay Antiproliferative activity against BCA2 and ER deficient human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 20222671]
MDA-MB-231	IC₅₀	0.32 μM Compound: 1, DSF	Antiproliferative activity against human MDA-MB-231 cells expressing BCA2 and ERalpha after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells expressing BCA2 and ERalpha after 72 hrs by MTT assay	[PMID: 20222671]
T47D	IC₅₀	0.17 μM Compound: 1, DSF	Antiproliferative activity against human T47D cells expressing BCA2 and estrogen receptor after 72 hrs by MTT assay Antiproliferative activity against human T47D cells expressing BCA2 and estrogen receptor after 72 hrs by MTT assay	[PMID: 20222671]

In Vitro

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 (0.1 nM-10 μM; 72 h) + Cu²⁺ combination enhances the cytotoxicity on ovarian cancer cell lines^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Disulfiram significantly inhibits the tumor growth (by 74%), associated with in vivo proteasome inhibition and apoptosis induction in mice bearing MDA-MB-231 tumor xenografts^[1].
Proteasome inhibition is measured by decreased levels of tumor tissue proteasome activity and accumulation of ubiquitinated proteins and natural proteasome substrates p27 and Bax^[1].
Apoptosis is shown by caspase activation and apoptotic nuclei formation^[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^[4].
Disulfiram inhibits growth and angiogenesis in melanomas transplanted in severe combined immunodeficient mice, and these effects are potentiated by Zn²⁺ supplementation^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

296.54

Formula

C₁₀H₂₀N₂S₄

CAS No.

97-77-8

Appearance

Solid

Color

White to yellow

SMILES

S=C(SSC(N(CC)CC)=S)N(CC)CC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : 75 mg/mL (252.92 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (7.01 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (7.01 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (7.01 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: Corn Oil
Solubility: 30 mg/mL (101.17 mM); Clear solution; Need ultrasonic
Protocol 2

Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 10 mg/mL (33.72 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.78%

Select Batch:

Data Sheet (280 KB) SDS (702 KB)

COA (0 KB) HNMR (256 KB) LCMS (267 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[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 [Content Brief]

[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.

[6]. Guo F, et, al. Inhibitory effect on ovarian cancer ALDH+ stem-like cells by Disulfiram and Copper treatment through ALDH and ROS modulation. Biomed Pharmacother. 2019 Oct;118:109371. [Content Brief]

Cell Assay ^[4]	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 HAuCl₄·3H₂O) 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). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[4]	Adult female CB17-SCID mice are housed in a protected laminar flow facility with access to water and either a standard diet containing 87 ppm zinc or a zinc-supplemented diet containing 1,000 ppm Zn²⁺ as zinc acetate. Mice are injected s.c. in the right groin with 5×10⁶ cells from a highly aggressive malignant melanoma obtained from a Carolinas Medical Center patient. The frozen tumor is passaged twice in SCID mice to adapt it to in vivo growth before use in these experiments. On the day of tumor injection, all mice began daily administration of drug. Drug is given in a total volume of 0.2 mL by gastric gavage via smooth Teflon-tipped needles inserted transorally into the stomach. Four groups are studied: tumor control (n=10; 0.2 mL olive oil daily; zinc diet of 87 ppm); zinc-supplemented control (n=10; 0.2 mL olive oil daily; zinc diet of 1,000 ppm); disulfiram (n=10; 200 mg/kg/d disulfiram in 0.2 mL olive oil; zinc diet of 87 ppm); and zinc-supplemented diet + disulfiram (n=10; 200 mg/kg/d disulfiram in 0.2 mL olive oil; zinc diet of 1,000 ppm). Mice are examined daily, the tumor is measured in two dimensions, and the tumor volume is estimated using the formula for an elipse. When estimated tumor volume approached 500 mm³ within any animal, all mice are euthanized. Tumors are excised, weighed, fixed in formalin, sectioned, and stained or immunostained for factor VIII. Slides are coded and examined by a blinded observer who identified vessels as deposits of red cells. For each slide, the number of vessels is counted in four different fields representative of the tumor. The average number of vessels per field is averaged per biopsy specimen and used to evaluate tumor vascularity. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. [Content Brief] [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. [Content Brief] [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. [Content Brief] [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 [Content Brief] [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. [6]. Guo F, et, al. Inhibitory effect on ovarian cancer ALDH+ stem-like cells by Disulfiram and Copper treatment through ALDH and ROS modulation. Biomed Pharmacother. 2019 Oct;118:109371. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.3722 mL	16.8611 mL	33.7223 mL	84.3057 mL
	5 mM	0.6744 mL	3.3722 mL	6.7445 mL	16.8611 mL
	10 mM	0.3372 mL	1.6861 mL	3.3722 mL	8.4306 mL
	15 mM	0.2248 mL	1.1241 mL	2.2482 mL	5.6204 mL
	20 mM	0.1686 mL	0.8431 mL	1.6861 mL	4.2153 mL
	25 mM	0.1349 mL	0.6744 mL	1.3489 mL	3.3722 mL
	30 mM	0.1124 mL	0.5620 mL	1.1241 mL	2.8102 mL
	40 mM	0.0843 mL	0.4215 mL	0.8431 mL	2.1076 mL
	50 mM	0.0674 mL	0.3372 mL	0.6744 mL	1.6861 mL
	60 mM	0.0562 mL	0.2810 mL	0.5620 mL	1.4051 mL
	80 mM	0.0422 mL	0.2108 mL	0.4215 mL	1.0538 mL
	100 mM	0.0337 mL	0.1686 mL	0.3372 mL	0.8431 mL

Disulfiram Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Disulfiram97-77-8Tetraethylthiuram disulfide TETDAldehyde Dehydrogenase (ALDH)Interleukin RelatedPyroptosisApoptosisCuproptosisILInhibitorinhibitorinhibit

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Disulfiram (Synonyms: Tetraethylthiuram disulfide; TETD)

Customer Review

Other Forms of Disulfiram:

Disulfiram Related Antibodies

87 Publications Citing Use of MCE Disulfiram

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Aldehyde Dehydrogenase (ALDH) Isoform Specific Products:

View All Interleukin Related Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Disulfiram Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Disulfiram Related Classifications

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