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Biological Activity for Disulfiram
Disulfiram is an inhibitor of aldehyde dehydrogenase that displays antialcoholism activity. Shown to reversibly stimulate Ca2+-ATPase activity and inhibit V-ATPase (EC50 = 26 μM). Also inhibits expression of MMP-2 and MMP-9 and displays anti-invasive activity. Pyroptosis inhibitor; binds gasdermin D (GSDMD) and inhibits pore formation. Also inhibits SARS-CoV-2 main protease (Mpro; IC50 = 9.35 μM) and inhibits viral replication in Vero cells in vitro.
Technical Data for Disulfiram
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Disulfiram
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for Disulfiram
The following data is based on the product molecular weight 296.54. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||3.37 mL||16.86 mL||33.72 mL|
|5 mM||0.67 mL||3.37 mL||6.74 mL|
|10 mM||0.34 mL||1.69 mL||3.37 mL|
|50 mM||0.07 mL||0.34 mL||0.67 mL|
References for Disulfiram
References are publications that support the biological activity of the product.
Starling et al (1996) Stimulation of the Ca2+-ATPase of sarcoplasmic reticulum by disul. Biochem.J. 320 101 PMID: 8947473
Cho et al (2007) Disulfiram suppresses invasive ability of osteosarcoma cells via the inhibition of MMP-2 and MMP-9 expression. J.Biochem.Mol.Biol. 40 1069 PMID: 18047805
Johnson et al (2009) Identification of inhibitors of vacuolar proton-translocating ATPase pumps in yeast by high-throughput screening flow cytometry. Anal.Biochem. 398 203 PMID: 20018164
Fisher et al (2010) The ethanol metabolite acetaldehyde increases paracellular drug permeability in vitro and oral bioavailability in vivo. J.Pharmacol.Exp.Ther. 332 326 PMID: 19820208
Pandeya et al (2019) Gasdermin D (GSDMD) as a new target for the treatment of infection. Medchemcomm 10 660 PMID: 31191857
Jin et al (2020) Structure of Mpro from SARS-CoV-2 and discovery of its inhibitors. Nature 582 289 PMID: 32272481
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Keywords: Disulfiram, Disulfiram supplier, aldehyde, dehydrogenase, inhibitors, inhibits, anti-alcoholism, stimulates, stimulators, reversible, ca2+-atpase, V-atpase, vacuolar, atpase, MMP, matrix, metalloproteinase, metalloprotease, MMP-2, MMP-9, proteinase, protease, pyroptosis, gasdermin, D, GSDMD, COVID-19, severe, acu, Tetraethylthiuram, disulfide, Aldehyde, Dehydrogenase, Ca2+-ATPase, H+-ATPase, Matrix, Metalloprotease, Inflammasomes, 3C, and, 3CL, Proteases, Coronavirus, 3807, Tocris Bioscience
3 Citations for Disulfiram
Citations are publications that use Tocris products. Selected citations for Disulfiram include:
Chan et al (2016) HIV-1 latency and virus production from unintegrated genomes following direct infection of resting CD4 T cells. PLoS One 13 1 PMID: 26728316
Ahadome et al (2016) Aldehyde dehydrogenase inhibition blocks mucosal fibrosis in human and mouse ocular scarring. JCI Insight 1 e87001 PMID: 27699226
Franz S et al (2020) A phenotypic screening platform utilising human spermatozoa identifies compounds with contraceptive activity. Elife 9 PMID: 31987071
Do you know of a great paper that uses Disulfiram from Tocris? Please let us know.
Reviews for Disulfiram
Average Rating: 5 (Based on 1 Review.)
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Recombinant Aldh1 was used in a standard fluorometric reporter assay with NAD+ as a cofactor, reaction velocity measured as relative changes in fluorescence. Disulfiram was added immediately prior to assessing activity. We noted decreasing velocity rates over time supporting this as a time-dependent/ irreversible inhibitor of Aldh enzymes.
Pre-incubation of recombinant enzyme will lead to full depletion of activity. Observed IC50 (initial) at approximately 50 uM.