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Disulfiram (NSC 190940)
Catalog No.S1680 Synonyms: Tetraethylthiuram disulfide, TETD
For research use only.
Disulfiram (NSC 190940, Tetraethylthiuram disulfide, TETD) 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).
CAS No. 97-77-8
Selleck's Disulfiram (NSC 190940) has been cited by 27 publications
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Biological Activity
| Description | Disulfiram (NSC 190940, Tetraethylthiuram disulfide, TETD) 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). | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| 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] |
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| Cell Data |
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| 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)
| References |
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Solubility (25°C)
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In vitro |
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In vivo |
Add solvents to the product individually and in order |
2.5mg/mL |
Chemical Information
| Molecular Weight | 296.54 | ||
|---|---|---|---|
| Formula | C10H20N2S4 |
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| CAS No. | 97-77-8 | ||
| Storage | 3 years | -20°C | powder |
| 2 years | -80°C | in solvent | |
| Smiles | CCN(CC)C(=S)SSC(=S)N(CC)CC | ||
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Clinical Trial Information
| NCT Number | Recruitment | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT04485130 | Recruiting | Drug: Disulfiram|Drug: Placebo | Covid19 | University of California San Francisco | May 1 2021 | Phase 2 |
| NCT03151772 | Terminated | Drug: Disulfiram|Drug: Metformin | Glioblastoma | Sahlgrenska University Hospital Sweden | January 29 2018 | Early Phase 1 |
| NCT02309801 | Completed | Dietary Supplement: Daidzin|Dietary Supplement: Alcohol | Healthy | Parc de Salut Mar|Ministerio de Sanidad Servicios Sociales e Igualdad | July 2012 | Phase 1 |
| NCT01286259 | Completed | Drug: Disulfiram | HIV-1 Infection | University of California San Francisco|Johns Hopkins University | January 2011 | Not Applicable |
| NCT02101008 | Completed | Drug: disulfiram and chelated zinc | Melanoma | University of Utah | March 2010 | Phase 2 |
(data from https://clinicaltrials.gov, updated on 2022-01-17)
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