Catalog No.S1680 Synonyms: NSC 190940
Molecular Weight(MW): 296.54
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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The effect of drugs on sperm movement. Purified human sperm were incubated under capacitating conditions for 0, 15, 30, 60 or 120 min, and motility was measured in the presence of disulfirum. The standard deviation is shown as bars. Statistical differences by Student's t-test compared with control are annotated as “*” for p<0.05 or “**” for p<0.01.
J Proteomics 2013 79, 114-22. Disulfiram purchased from Selleck.
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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
|Description||Disulfiram is a specific inhibitor of aldehyde-dehydrogenase (ALDH1), used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol.|
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.  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.  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.  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. 
|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.  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. |
|In vitro||DMSO||59 mg/mL (198.96 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.
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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02678975||Not yet recruiting||Glioma|Glioblastoma||Sahlgrenska University Hospital, Sweden|St. Olavs Hospital|Lund University Hospital|Karolinska University Hospital||September 2016||Phase 2|
|NCT02770378||Not yet recruiting||Glioblastoma||University of Ulm|Reliable Cancer Therapies|Anticancer Fund, Belgium||August 2016||Phase 1|
|NCT02715609||Not yet recruiting||Glioblastoma Multiforme||Washington University School of Medicine|University of Calgary||June 2016||Phase 1|Phase 2|
|NCT02735577||Recruiting||Alcohol Use Disorder||New York State Psychiatric Institute||March 2016||Phase 4|
|NCT02671890||Recruiting||Metastatic Pancreatic Adenocarcinoma|Recurrent Pancreatic Carcinoma|Solid Neoplasm|Stage IV Pancreatic Cancer||Mayo Clinic|National Cancer Institute (NCI)||February 2016||Phase 1|
|NCT01777919||Not yet recruiting||Glioblastoma Multiforme||Olympion Medical Center|University of Ioannina|University of Eastern Finland|University of Ulm||September 2015||Phase 2|
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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