Disulfiram

製品コードS1680 バッチS168002

化学情報

	Synonyms	NSC 190940, Tetraethylthiuram disulfide, TETD	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₀H₂₀N₂S₄
	分子量	296.54	CAS No.	97-77-8
Solubility (25°C)*	体外	DMSO	59 mg/mL (198.96 mM)
		Ethanol	59 mg/mL (198.96 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Disulfiram is a specific inhibitor of aldehyde-dehydrogenase (ALDH) with IC50 of 0.15 μM and 1.45 μM for hALDH1 and hALDH2, respectively. Disulfiram is used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram induces apoptosis. Disulfiram is also an inhibitor of pore formation by gasdermin D (GSDMD).
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. ^[1] Disulfiram (DS), a clinically used anti-alcoholism drug, strongly inhibits constitutive and 5-FU-induced NF-kappaB activity in a dose-dependent manner. Disulfiram inhibits both NF-kappaB nuclear translocation and DNA binding activity but has no effect on 5-FU-induced IkappaBalpha degradation. Disulfiram 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. Disulfiram also effectively abolishes 5-FU chemoresistance in a 5-FU resistant cell line H630(5-FU) in vitro. ^[2] 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. ^[3] Disulfiram 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. ^[4]
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. ^[1] Disulfiram 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. Disulfiram inhibits growth and angiogenesis in melanomas transplanted in severe combined immunodeficient mice, and these effects are potentiated by Zn2+ supplementation. ^[4]

製品説明

Disulfiram is a specific inhibitor of aldehyde-dehydrogenase (ALDH) with IC50 of 0.15 μM and 1.45 μM for hALDH1 and hALDH2, respectively. Disulfiram is used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram induces apoptosis. Disulfiram is also an inhibitor of pore formation by gasdermin D (GSDMD).

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. ^[1]

Disulfiram (DS), a clinically used anti-alcoholism drug, strongly inhibits constitutive and 5-FU-induced NF-kappaB activity in a dose-dependent manner. Disulfiram inhibits both NF-kappaB nuclear translocation and DNA binding activity but has no effect on 5-FU-induced IkappaBalpha degradation. Disulfiram 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. Disulfiram also effectively abolishes 5-FU chemoresistance in a 5-FU resistant cell line H630(5-FU) in vitro. ^[2]

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. ^[3]

Disulfiram 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. ^[4]

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. ^[1]

Disulfiram 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. Disulfiram inhibits growth and angiogenesis in melanomas transplanted in severe combined immunodeficient mice, and these effects are potentiated by Zn2+ supplementation. ^[4]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	MDA-MB-231 cells
	濃度	20 μM
	反応時間	24 h
	実験の流れ	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 DSF or TM or vehicle DMSO for 24 hours.
動物実験	動物モデル	Female athymic nude mice
	投薬量	50 mg/kg
	投与方法

参考

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カスタマーフィードバック

: Data from [J Proteomics, 2013, 79, 114-22]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

The TRIM21-FOXD1-BCL-2 axis underlies hyperglycaemic cell death and diabetic tissue damage [ Cell Death Dis, 2023, 14(12):825]	PubMed: 38092733
CEBPG suppresses ferroptosis through transcriptional control of SLC7A11 in ovarian cancer [ J Transl Med, 2023, 21(1):334]	PubMed: 37210575
PANoptosis-like cell death in ischemia/reperfusion injury of retinal neurons [ Neural Regen Res, 2023, 18(2):357-363]	PubMed: 35900430
PKR deficiency delays vascular aging via inhibiting GSDMD-mediated endothelial cell hyperactivation [ iScience, 2023, 26(1):105909]	PubMed: 36691613
BAK-Mediated Pyroptosis Promotes Japanese Encephalitis Virus Proliferation in Porcine Kidney 15 Cells [ Viruses, 2023, 15(4)974]	PubMed: 37112954
Reconstitution of human pyroptotic cell death in Saccharomyces cerevisiae [ Sci Rep, 2023, 13(1):3095]	PubMed: 36813876
Lack of impact of the ALDH2 rs671 variant on breast cancer development in Japanese BRCA1/2-mutation carriers [ Cancer Med, 2023, 12(6):6594-6602]	PubMed: 36345163
HMGB2 causes photoreceptor death via down-regulating Nrf2/HO-1 and up-regulating NF-κB/NLRP3 signaling pathways in light-induced retinal degeneration model [ Free Radic Biol Med, 2022, 181:14-28]	PubMed: 35091064
Coronaviruses Nsp5 Antagonizes Porcine Gasdermin D-Mediated Pyroptosis by Cleaving Pore-Forming p30 Fragment [ mBio, 2022, 10.1128/mbio.02739-21]	PubMed: 35012343
Disulfiram inhibits IL-1β secretion and inflammatory cells recruitment in Aspergillus fumigatus keratitis [ Int Immunopharmacol, 2022, 102:108401]	PubMed: 34883353

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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