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Description: Reversibly stimulates SERCA Ca2+-ATPase; displays a range of other activities
Alternative Names: Tetraethylthiuram disulfide
Chemical Name: Bis(diethylthiocarbamyoyl)disulfide
Citations (3)
Reviews (1)

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

M. Wt 296.54
Formula C10H20N2S4
Storage Store at +4°C
CAS Number 97-77-8
PubChem ID 3117

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
DMSO 5.93 20
ethanol 29.65 100

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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets for Disulfiram

Certificate of Analysis / Product Datasheet
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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

If you know of a relevant reference for Disulfiram, please let us know.

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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

Franz S et al (2020) A phenotypic screening platform utilising human spermatozoa identifies compounds with contraceptive activity. Elife 9 PMID: 31987071

Ahadome et al (2016) Aldehyde dehydrogenase inhibition blocks mucosal fibrosis in human and mouse ocular scarring. JCI Insight 1 e87001 PMID: 27699226

Do you know of a great paper that uses Disulfiram from Tocris? Please let us know.

Reviews for Disulfiram

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Irreversible inhibitor of Aldh1 with IC50 initial at 50 uM.
By Anonymous on 10/26/2019
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: recombinant mouse Aldh1

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.

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