| Size | Price | Stock | Qty |
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| 250mg |
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| 10g |
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| 25g |
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Purity: ≥98%
Disulfiram (Disulfan; NSC 190940; Dicupral; Disetil; NSC190940; Tetraethylthiuram disulfide; TETD) is a potent and specific inhibitor of aldehyde-dehydrogenase (ALDH1) that is used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. The mechanism of action of disulfiram is to block the metabolic processing of alcohol in the body by inhibiting acetaldehyde dehydrogenase (coverts acetaldehyde to acetic acid), thus causing unpleasant effects when even a small amount of alcohol is consumed.
| ln Vitro |
Disulfiram-copper complex efficiently reduces proteasome activity in cultured breast cancer MDA-MB-231 and MCF10DCIS.com cells prior to causing apoptotic cancer cell death, but not in normal immortalized MCF-10A cells [1]. A commercially utilized anti-alcoholic medication called disulfiram (DS) significantly and dose-dependently suppresses both constitutive and 5-FU-induced NF-activation. DisuLfiram has little effect on 5-FU-induced IkappaBalpha degradation, although it does reduce NF-kappaB nuclear translocation and DNA binding activity. Disulfiram synergistically increased 5-FU's cytotoxicity on both DLD-1 and RKO (WT) cell lines while also markedly enhancing 5-FU's apoptotic effect on those lines. Additionally, 5-FU chemoresistance in the 5-FU-resistant cell line H630 (5-FU) is successfully eliminated in vitro by DisuLfiram [2]. CuCl2 greatly increased DSF-induced cell death to less than 10% of the control, while oseltamivir decreased the number of viable cells [3]. At lower concentrations than disulfiram alone, disulfiram in combination with Cu2+ or Zn2+ in melanoma cells decreases cyclin A expression and inhibits in vitro proliferation [4]. The combination of DisuLfiram (0.1 nM-10 μM; 72 h) and Cu2+ increases its cytotoxicity against ovarian cancer cell lines [1].
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| ln Vivo |
Disulfiram dramatically reduced tumor development (74%) in mice containing MDA-MB-231 tumor xenografts; this was linked to proteasome inhibition and apoptosis induction [1]. In tumor tissues, ubiquitinated proteins and the natural proteasome substrates p27 and Bax accumulate, and these indicators of proteasome inhibition are used to gauge the extent of proteasome suppression. Caspases being activated and apoptotic cell nuclei forming are signs of apoptosis [1]. Disulfiram inhibits the nuclear factor-kappaB transcription factor, limits the P-glycoprotein extrusion pump, decreases angiogenesis, makes tumors more susceptible to chemotherapy, and stops tumor growth in mice [4]. When melanoma tumors are transplanted into severe combined immunodeficient mice, disulfiram reduces their development and angiogenesis; Zn2+ supplementation amplifies these effects [4].
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| References |
[1]. Chen D, ert al. 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.
[2]. Wang W, et al. Disulfiram-mediated inhibition of NF-kappaB activity enhances cytotoxicity of 5-fluorouracil in human colorectal cancer cell lines. Int J Cancer. 2003 Apr 20;104(4):504-11. [3]. Cen D, et al. Disulfiram facilitates intracellular Cu uptake and induces apoptosis in human melanoma cells. J Med Chem. 2004 Dec 30;47(27):6914-20. [4]. Brar SS, et al. Disulfiram inhibits activating transcription factor/cyclic AMP-responsive element binding protein and human melanoma growth in a metal-dependent manner in vitro, in mice and in a patient with metastatic disease. Mol Cancer Ther. 2004 Sep;3 [5]. Jun Jacob Hu, et al. Identification of pyroptosis inhibitors that target a reactive cysteine in gasdermin D. The Preprint Server For Biology, 2018,Jul. 10. [6]. Guo F, et, al. Inhibitory effect on ovarian cancer ALDH+ stem-like cells by Disulfiram and Copper treatment through ALDH and ROS modulation. Biomed Pharmacother. 2019 Oct;118:109371 |
| Molecular Formula |
C10H20N2S4
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| Molecular Weight |
296.54
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| CAS # |
97-77-8
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| SMILES |
S=C(SSC(N(CC)CC)=S)N(CC)CC
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3722 mL | 16.8611 mL | 33.7223 mL | |
| 5 mM | 0.6744 mL | 3.3722 mL | 6.7445 mL | |
| 10 mM | 0.3372 mL | 1.6861 mL | 3.3722 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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