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Disulfiram

Catalog No.
A4015
Dopamine β-hydroxylase inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$55.00
In stock
1g
$47.00
In stock
5g
$67.00
In stock

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Background

Disulfiram blocks the processing of alcohol in the body by inhibiting acetaldehyde dehydrogenase thus causing an unpleasant reaction when alcohol is consumed.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt296.54
Cas No.97-77-8
FormulaC10H20N2S4
Solubility≥12 mg/mL in DMSO, ≥24.2 mg/mL in EtOH with ultrasonic,insoluble in H2O
Chemical Namediethylcarbamothioylsulfanyl N,N-diethylcarbamodithioate
SDFDownload SDF
Canonical SMILESCCN(CC)C(=S)SSC(=S)N(CC)CC
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Protocol

Kinase experiment [1]:

Binding assays

The chymotrypsin-like activity of purified 20S proteasome was measured. Briefly, 17.5 ng of purified 20S proteasome were incubated in 100 μL of assay buffer (50 mmol/L Tris-HCl, pH 7.5) with or without different concentrations of copper chloride, Disulfiram, or the Disulfiram-copper mixture and 10 μmol/L fluorogenic peptide substrate Suc-LLVY-AMC (for the proteasomal chymotrypsin-like activity) for 2 hrs at 37℃. After incubation, production of hydrolyzed AMC groups was measured with a Wallac Victor3 multilabel counter with an excitation filter of 365 nm and an emission filter of 460 nm.

Cell experiment [1]:

Cell lines

MDA-MB-231 cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

5 ~ 20 μM; 24 hrs

Applications

The Disulfiram-copper complex potently inhibited the proteasomal activity in cultured breast cancer MDA-MB-231 cells, before induction of apoptotic cancer cell death.

Animal experiment [1]:

Animal models

Mice bearing MDA-MB-231 tumor xenografts

Dosage form

50 mg/kg/d; p.o.; 29 days

Applications

In mice bearing MDA-MB-231 tumor xenografts, Disulfiram significantly inhibited tumor growth (by 74%), associated with in vivo proteasome inhibition and apoptosis induction.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Chen D, Cui QC, Yang H, Dou QP. Disulfiram, a clinically used anti-alcoholism drug and copper-binding agent, induces apoptotic cell death in breast cancer cultures and xenografts via inhibition of the proteasome activity. Cancer Res. 2006 Nov 1;66(21):10425-33.

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