Disulfiram

Catalog No.S1680
5 5 2 Product Citations

Disulfiram is a specific inhibitor of aldehyde-dehydrogenase (ALDH1), used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol.

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In DMSO USD 130 In stock
USD 97 In stock
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Disulfiram  Chemical Structure

Disulfiram Chemical Structure
Molecular Weight: 296.54

Validation & Quality Control

Customer Reviews(1)

Quality Control & MSDS

Related Compound Libraries

Disulfiram is available in the following compound libraries:

Product Information

Product Description

Biological Activity

Description Disulfiram is a specific inhibitor of aldehyde-dehydrogenase (ALDH1), used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol.
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]
Features

Protocol(Only for Reference)

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Chen D, et al. Cancer Res, 2006, 66(21), 10425-10433.

[2] Wang W, et al. Int J Cancer, 2003, 104(4), 504-511.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2014-11-22)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT01777919 Not yet recruiting Glioblastoma Multiforme Olympion Medical Center|University of Ioannina|University  ...more Olympion Medical Center|University of Ioannina|University of Eastern Finland|University of Ulm September 2015 Phase 2
NCT02134002 Not yet recruiting Cocaine Dependence Assistance Publique - Hôpitaux de Paris|National Research  ...more Assistance Publique - Hôpitaux de Paris|National Research Agency, France June 2014 Phase 4
NCT01907165 Recruiting Glioblastoma Washington University School of Medicine October 2013 --
NCT01944371 Completed HIV|Human Immunodeficiency Virus University of California, San Francisco|Monash University  ...more University of California, San Francisco|Monash University|amfAR, The Foundation for AIDS Research|National Institute of Allergy and Infectious Diseases (NIAID) August 2013 Phase 1|Phase 2
NCT01286259 Completed HIV-1 Infection University of California, San Francisco|Johns Hopkins Uni  ...more University of California, San Francisco|Johns Hopkins University January 2011 --

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Chemical Information

Download Disulfiram SDF
Molecular Weight (MW) 296.54
Formula

C10H20N2S4

CAS No. 97-77-8
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms
Solubility (25°C) * In vitro DMSO 59 mg/mL (198.96 mM)
Water <1 mg/mL (<1 mM)
Ethanol 59 mg/mL (198.96 mM)
* <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.
Chemical Name N,​N,​N',​N'-​tetraethyl-thioperoxydicarbonic diamide([(H2N)​C(S)​]​2S2)

Research Area

Customer Reviews (1)


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Rating
Source J Proteomics, 2013, 79:114-22. Disulfiram purchased from Selleck
Method Motility Assay
Cell Lines human sperm
Concentrations 10-80 uM
Incubation Time 0, 15, 30, 60 or 120 min
Results Disulfiram inhibited sperm motility.

Product Citations (2)

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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