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Disulfiram

Cat. No. 3807 3 篇引用文献 1 条评论 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Reversibly stimulates SERCA Ca2+-ATPase; displays a range of other activities
别名： Tetraethylthiuram disulfide
化学名： Bis(diethylthiocarbamyoyl)disulfide
说明书
引用文献 (3)
评论 (1)
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for Disulfiram

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

技术数据 for Disulfiram

分子量 296.54
公式 C10H20N2S4
储存 Store at +4°C
CAS Number 97-77-8
PubChem ID 3117
InChI Key AUZONCFQVSMFAP-UHFFFAOYSA-N
Smiles S=C(SSC(N(CC)CC)=S)N(CC)CC

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for Disulfiram

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 5.93 20
ethanol 29.65 100

制备储备液 for Disulfiram

以下数据基于产品分子量 296.54。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 3.37 mL 16.86 mL 33.72 mL
5 mM 0.67 mL 3.37 mL 6.74 mL
10 mM 0.34 mL 1.69 mL 3.37 mL
50 mM 0.07 mL 0.34 mL 0.67 mL

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产品说明书 for Disulfiram

分析证书/产品说明书
选择另一批次：
化学品安全技术说明书

参考文献 for Disulfiram

参考文献是支持产品生物活性的出版物。

Starling et al (1996) Stimulation of the Ca2+-ATPase of sarcoplasmic reticulum by disul. Biochem.J. 320 101 PMID: 8947473

Cho et al (2007) Disulfiram suppresses invasive ability of osteosarcoma cells via the inhibition of MMP-2 and MMP-9 expression. J.Biochem.Mol.Biol. 40 1069 PMID: 18047805

Johnson et al (2009) Identification of inhibitors of vacuolar proton-translocating ATPase pumps in yeast by high-throughput screening flow cytometry. Anal.Biochem. 398 203 PMID: 20018164

Fisher et al (2010) The ethanol metabolite acetaldehyde increases paracellular drug permeability in vitro and oral bioavailability in vivo. J.Pharmacol.Exp.Ther. 332 326 PMID: 19820208

Pandeya et al (2019) Gasdermin D (GSDMD) as a new target for the treatment of infection. Medchemcomm 10 660 PMID: 31191857

Jin et al (2020) Structure of Mpro from SARS-CoV-2 and discovery of its inhibitors. Nature 582 289 PMID: 32272481

If you know of a relevant reference for Disulfiram, please let us know.

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关键词: Disulfiram, Disulfiram supplier, aldehyde, dehydrogenase, inhibitors, inhibits, anti-alcoholism, stimulates, stimulators, reversible, ca2+-atpase, V-atpase, vacuolar, atpase, MMP, matrix, metalloproteinase, metalloprotease, MMP-2, MMP-9, proteinase, protease, pyroptosis, gasdermin, D, GSDMD, COVID-19, severe, acu, Tetraethylthiuram, disulfide, Aldehyde, Dehydrogenase, Ca2+-ATPase, H+-ATPase, Matrix, Metalloprotease, Inflammasomes, 3C, and, 3CL, Proteases, Coronavirus, 3807, Tocris Bioscience

3 篇 Disulfiram 的引用文献

引用文献是使用了 Tocris 产品的出版物。 Disulfiram 的部分引用包括：

Chan et al (2016) HIV-1 latency and virus production from unintegrated genomes following direct infection of resting CD4 T cells. PLoS One 13 1 PMID: 26728316

Franz S et al (2020) A phenotypic screening platform utilising human spermatozoa identifies compounds with contraceptive activity. Elife 9 PMID: 31987071

Ahadome et al (2016) Aldehyde dehydrogenase inhibition blocks mucosal fibrosis in human and mouse ocular scarring. JCI Insight 1 e87001 PMID: 27699226

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Disulfiram 的评论

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Irreversible inhibitor of Aldh1 with IC50 initial at 50 uM.
By Anonymous on 10/26/2019
分析类型： In Vitro
种属： Mouse
细胞系/组织： recombinant mouse Aldh1

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.

Pre-incubation of recombinant enzyme will lead to full depletion of activity. Observed IC50 (initial) at approximately 50 uM.

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