Tetraethylthiuram disulfide (Disulfiram)

Katalognr.S1680 Batch:S168003

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Tekniska data

Formel

C10H20N2S4
Molekylvikt 296.54 CAS-nr. 97-77-8
Löslighet (25°C)* In vitro DMSO 59 mg/mL (198.96 mM)
Water Insoluble
Ethanol Insoluble
In Vivo (Tillsätt lösningsmedel till produkten individuellt och i ordning.)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO Corn oil

Validerad av Selleck-laboratorier. Om du behöver justeringar av denna formulering, kontakta vårt säljteam för skräddarsydd testning.

 5.000mg/ml (16.86mM) Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

Validerad av Selleck-laboratorier. Om du behöver justeringar av denna formulering, kontakta vårt säljteam för skräddarsydd testning.

 3.900mg/ml (13.15mM) Taking the 1 mL working solution as an example, add 50 μL of 78 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml betyder svårlösligt eller olösligt.
* Vänligen notera att Selleck testar lösligheten för alla förbindelser internt, och den faktiska lösligheten kan skilja sig något från publicerade värden. Detta är normalt och beror på små variationer mellan olika partier.
* Rumstempererad frakt (Stabilitetstester visar att denna produkt kan fraktas utan några kylåtgärder.)

Beredning av stamlösningar

Biologisk aktivitet

Beskrivning Disulfiram är en specifik hämmare av aldehyddehydrogenas (ALDH) med IC50 på 0,15 μM och 1,45 μM för hALDH1 respektive hALDH2. Disulfiram används för behandling av kronisk alkoholism genom att producera en akut känslighet för alkohol. Disulfiram inducerar apoptos. Disulfiram är också en hämmare av porbildning av gasdermin D (GSDMD).
Mål
ALDH1
(Cell-free assay)		 ALDH2
(Cell-free assay)
0.15 μM 1.45 μM
In vitro

Disulfiram-copper complex potently inhibits the proteasomal activity in cultured breast cancer MDA-MB-231 and MCF10DCIS.com cells, but not normal, immortalized MCF-10A cells, before induction of apoptotic cancer cell death.

This compound (DS), a clinically used anti-alcoholism drug, strongly inhibits constitutive and 5-FU-induced NF-kappaB activity in a dose-dependent manner. It inhibits both NF-kappaB nuclear translocation and DNA binding activity but has no effect on 5-FU-induced IkappaBalpha degradation. This chemical significantly enhances the apoptotic effect of 5-FU on DLD-1 and RKO(WT) cell lines and synergistically potentiated the cytotoxicity of 5-FU to both cell lines. It also effectively abolishes 5-FU chemoresistance in a 5-FU resistant cell line H630(5-FU) in vitro.

Oseltamivir decreases the number of viable cells, and the addition of CuCl(2) significantly enhances the DSF-induced cell death to less than 10% of control.

This compound given to melanoma cells in combination with Cu2+ or Zn2+ decreases expression of cyclin A and reduces proliferation in vitro at lower concentrations than disulfiram alone.

In Vivo

Disulfiram significantly inhibits the tumor growth (by 74%), associated with in vivo proteasome inhibition (as measured by decreased levels of tumor tissue proteasome activity and accumulation of ubiquitinated proteins and natural proteasome substrates p27 and Bax) and apoptosis induction (as shown by caspase activation and apoptotic nuclei formation) in mice bearing MDA-MB-231 tumor xenografts.

This compound blocks the P-glycoprotein extrusion pump, inhibits the transcription factor nuclear factor-kappaB, sensitizes tumors to chemotherapy, reduces angiogenesis, and inhibits tumor growth in mice. It inhibits growth and angiogenesis in melanomas transplanted in severe combined immunodeficient mice, and these effects are potentiated by Zn2+ supplementation.

Protokoll (från referens)

Cellanalys:

[1]
  • Cellinjer

    MDA-MB-231 cells

  • Koncentrationer

    20 μM

  • Inkubationstid

    24 h

  • Metod

    Cells cultured in medium containing 25 µM copper for 3 days and then maintained in normal growth medium (without additional copper) were treated with 20 µM this compound or TM or vehicle DMSO for 24 hours.

Referenser

  • https://pubmed.ncbi.nlm.nih.gov/17079463/
  • https://pubmed.ncbi.nlm.nih.gov/12584750/
  • https://pubmed.ncbi.nlm.nih.gov/15615540/
  • https://pubmed.ncbi.nlm.nih.gov/15367699/
  • https://pubmed.ncbi.nlm.nih.gov/9354647/
  • https://pubmed.ncbi.nlm.nih.gov/32367036/

Kundvalidering av produkt

<p>The effect of drugs on sperm movement. Purified human sperm were incubated under capacitating conditions for 0, 15, 30, 60 or 120 min, and motility was measured in the presence of disulfirum. The standard deviation is shown as bars. Statistical differences by Student's t-test compared with control are annotated as “*” for p<0.05 or “**” for p<0.01.</p>

Data från [ J Proteomics , 2013 , 79, 114-22 ]

Sellecks Tetraethylthiuram disulfide (Disulfiram) Har citerats av 54 Publikationer

Statins targeting mevalonate-geranylgeranyl diphosphate pathway inhibit proliferation in NK/T lymphoma by promoting pyroptosis [ Transl Oncol, 2026, 67:102747] PubMed: 41932011
Disulfiram/Copper Combination as a Potential Therapeutic Approach for Hepatocellular Carcinoma: Targeting the ATF3-Mitochondrial Cell Death Pathway [ J Cancer, 2026, 17(1):117-130] PubMed: 41438581
Disulfiram/Copper Combination as a Potential Therapeutic Approach for Hepatocellular Carcinoma: Targeting the ATF3-Mitochondrial Cell Death Pathway [ Journal of Cancer, 2026, 117-130] PubMed: 41438581
Prefoldin complex promotes interferon-stimulated gene expression and is inhibited by rotavirus VP3 [ Nat Commun, 2025, 16(1):8083] PubMed: 40883306
Targeting USP21 to inhibit abdominal aortic aneurysm progression by suppressing the phenotypic transition of vascular smooth muscle cells [ Cell Rep Med, 2025, 6(9):102328] PubMed: 40925375
ADH5/ALDH2 dehydrogenases and DNA polymerase theta protect normal and malignant hematopoietic cells from formaldehyde challenge: therapeutic implications [ Leukemia, 2025, 39(9):2152-2162] PubMed: 40640557
Exploiting mitochondrial dysfunction to overcome BRAF inhibitor resistance in advanced melanoma: the role of disulfiram as a copper ionophore [ Cell Death Dis, 2025, 16(1):482] PubMed: 40592836
HOXC8 impacts lung tumorigenesis by preventing pyroptotic cell death through the suppression of caspase-1 expression [ Cell Death Dis, 2025, 16(1):552] PubMed: 40701951
Inhibition of NLRP3 enhances pro-apoptotic effects of FLT3 inhibition in AML [ Cell Commun Signal, 2025, 23(1):53] PubMed: 39875995
miR-126-5p protects from URSA via inhibiting Caspase-1-dependent pyroptosis of trophoblast cells [ Cell Mol Life Sci, 2025, 82(1):204] PubMed: 40372489

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