Disulfiram

Biological Activity

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 (M^pro; IC₅₀ = 9.35 μM) and inhibits viral replication in Vero cells in vitro.

Technical Data

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.

Background References

1. Disulfiram suppresses invasive ability of osteosarcoma cells via the inhibition of MMP-2 and MMP-9 expression.
   Cho et al.
   J.Biochem.Mol.Biol., 2007;40:1069
2. Identification of inhibitors of vacuolar proton-translocating ATPase pumps in yeast by high-throughput screening flow cytometry.
   Johnson et al.
   Anal.Biochem., 2009;398:203
3. The ethanol metabolite acetaldehyde increases paracellular drug permeability in vitro and oral bioavailability in vivo.
   Fisher et al.
   J.Pharmacol.Exp.Ther., 2010;332:326
4. Stimulation of the Ca²⁺-ATPase of sarcoplasmic reticulum by disul.
   Starling et al.
   Biochem.J., 1996;320:101
5. Gasdermin D (GSDMD) as a new target for the treatment of infection.
   Pandeya et al.
   Medchemcomm, 2019;10:660
6. Structure of M^pro from SARS-CoV-2 and discovery of its inhibitors.
   Jin et al.
   Nature, 2020;582:289

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