Chemical Name: Bis(diethylthiocarbamyoyl)disulfide
Biological ActivityDisulfiram 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Disulfiram suppresses invasive ability of osteosarcoma cells via the inhibition of MMP-2 and MMP-9 expression.
Cho et al.
Identification of inhibitors of vacuolar proton-translocating ATPase pumps in yeast by high-throughput screening flow cytometry.
Johnson et al.
The ethanol metabolite acetaldehyde increases paracellular drug permeability in vitro and oral bioavailability in vivo.
Fisher et al.
Stimulation of the Ca2+-ATPase of sarcoplasmic reticulum by disul.
Starling et al.
Gasdermin D (GSDMD) as a new target for the treatment of infection.
Pandeya et al.
Structure of Mpro from SARS-CoV-2 and discovery of its inhibitors.
Jin et al.
Citations for Disulfiram
The citations listed below are publications that use Tocris products. Selected citations for Disulfiram include:
2 Citations: Showing 1 - 2
Aldehyde dehydrogenase inhibition blocks mucosal fibrosis in human and mouse ocular scarring.
Authors: Ahadome Et al.
JCI Insight 2016;1:e87001
HIV-1 latency and virus production from unintegrated genomes following direct infection of resting CD4 T cells.
Authors: Chan Et al.
PLoS One 2016;13:1
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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.