2. Metabolic Enzyme/Protease Immunology/Inflammation Apoptosis
  3. Aldehyde Dehydrogenase (ALDH) Interleukin Related Pyroptosis Apoptosis Cuproptosis
  4. Disulfiram

Disulfiram  (Synonyms: Tetraethylthiuram disulfide; TETD)

Cat. No.: HY-B0240 Purity: 99.78%
SDS
COA
Handling Instructions Technical Support

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

Disulfiram Chemical Structure

CAS No. : 97-77-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
100 mg In-stock
500 mg In-stock
1 g In-stock
5 g In-stock
10 g   Get quote  
50 g   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 87 publication(s) in Google Scholar

Other Forms of Disulfiram:

Disulfiram Related Antibodies

Top Publications Citing Use of Products

87 Publications Citing Use of MCE Disulfiram

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

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[1][2][3][4][5][6].

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.

Disulfiram Related Antibodies
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.
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
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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

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)

g

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%

SDS (702 KB)

COA (244 KB) HNMR (256 KB) LCMS (267 KB)

Handling Instructions (2659 KB)
References
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

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.

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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

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

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Disulfiram
Cat. No.:
HY-B0240
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (702 KB) Français - FR (702 KB) Deutsch - DE (702 KB) Norwegian - NO (702 KB) Español - ES (702 KB) Swedish - SV (702 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.