Disulfiram

Catalog No.S1680 Batch:S168005

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Technical Data

Formula

C10H20N2S4
Molecular Weight 296.54 CAS No. 97-77-8
Solubility (25°C)* In vitro DMSO 59 mg/mL (198.96 mM)
Ethanol 59 mg/mL (198.96 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
10%DMSO 40%PEG300 5%Tween80 45%ddH2O
4.0mg/ml Taking the 1 mL working solution as an example, add 100 μL of 40 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 450 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Disulfiram is a specific inhibitor of aldehyde-dehydrogenase (ALDH) with IC50 of 0.15 μM and 1.45 μM for hALDH1 and hALDH2, respectively. Disulfiram is used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram induces apoptosis. Disulfiram is also an inhibitor of pore formation by gasdermin D (GSDMD).
Targets
ALDH1 [5]
(Cell-free assay)		 ALDH2 [5]
(Cell-free assay)
0.15 μM 1.45 μM
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 CuCl(2) 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]
In vivo

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]

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    MDA-MB-231 cells

  • Concentrations

    20 μM

  • Incubation Time

    24 h

  • Method

    Cells cultured in medium containing 25 µM copper for 3 days and then maintained in normal growth medium (without additional copper) were treated with 20 µM DSF or TM or vehicle DMSO for 24 hours.

Customer Product Validation

Data from [J Proteomics, 2013, 79, 114-22]

Selleck's Disulfiram has been cited by 39 publications

The TRIM21-FOXD1-BCL-2 axis underlies hyperglycaemic cell death and diabetic tissue damage [ Cell Death Dis, 2023, 14(12):825] PubMed: 38092733
CEBPG suppresses ferroptosis through transcriptional control of SLC7A11 in ovarian cancer [ J Transl Med, 2023, 21(1):334] PubMed: 37210575
PANoptosis-like cell death in ischemia/reperfusion injury of retinal neurons [ Neural Regen Res, 2023, 18(2):357-363] PubMed: 35900430
PKR deficiency delays vascular aging via inhibiting GSDMD-mediated endothelial cell hyperactivation [ iScience, 2023, 26(1):105909] PubMed: 36691613
BAK-Mediated Pyroptosis Promotes Japanese Encephalitis Virus Proliferation in Porcine Kidney 15 Cells [ Viruses, 2023, 15(4)974] PubMed: 37112954
Reconstitution of human pyroptotic cell death in Saccharomyces cerevisiae [ Sci Rep, 2023, 13(1):3095] PubMed: 36813876
Lack of impact of the ALDH2 rs671 variant on breast cancer development in Japanese BRCA1/2-mutation carriers [ Cancer Med, 2023, 12(6):6594-6602] PubMed: 36345163
HMGB2 causes photoreceptor death via down-regulating Nrf2/HO-1 and up-regulating NF-κB/NLRP3 signaling pathways in light-induced retinal degeneration model [ Free Radic Biol Med, 2022, 181:14-28] PubMed: 35091064
Coronaviruses Nsp5 Antagonizes Porcine Gasdermin D-Mediated Pyroptosis by Cleaving Pore-Forming p30 Fragment [ mBio, 2022, 10.1128/mbio.02739-21] PubMed: 35012343
Disulfiram inhibits IL-1β secretion and inflammatory cells recruitment in Aspergillus fumigatus keratitis [ Int Immunopharmacol, 2022, 102:108401] PubMed: 34883353

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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