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- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
Disulfiram
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
97-77-8
- 规格：
1g
是特异性的乙醛脱氢酶1型抗体 (ALDH1) 抑制剂。
【本资料源自公开渠道，如需（此处）屏蔽，请联系删除】
标题:Disulfiram-loaded copper sulfide nanoparticles for potential anti-glioma therapy
成员:Qing-Hua Lan, Chu-Chu Du, Run-Jie Yu, Jiaoyuan Zhai, Yannan Shi, Longfa Kou, Jian Xiao, Cui-Tao Lu, Ying-Zheng Zhao, Qing Yao
论文因子:5.875 发表期刊:INTERNATIONAL JOURNAL OF PHARMACEUTICS pmid:34371152
【本资料源自公开渠道，如需（此处）屏蔽，请联系删除】
标题:An Intrinsically Nontrimerizing Peptide Probe for Specifically Targeting Pathological Collagen in Connective Tissues
成员:Cai Xiangdong;Wei Wenyu;Bi Yihui; Liu Zhao;Bai Zh
论文因子:17.093 发表期刊:Advanced Functional Materials
| 基本信息 | |
| CAS | No.97-77-8 |
| 中文名称 | 二硫化四乙基秋兰姆 |
| 英文名称 | Disulfiram |
| 别名 | NSC 190940;双硫伦;TETD;Tetraethylthiuram disulfide |
| 分子式 | C10H20N2S4 |
| 分子量 | 296.54 |
| 溶解性 | Soluble in DMSO ≥10mg/mL |
| 纯度 | HPLC≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| EC | EINECS 202-607-8 |
| MDL | MFCD00009048 |
| SMILES | S=C(SSC(N(CC)CC)=S)N(CC)CC |
| InChIKey | AUZONCFQVSMFAP-UHFFFAOYSA-N |
| InChI | InChI=1S/C10H20N2S4/c1-5-11(6-2)9(13)15-16-10(14)12(7-3)8-4/h5-8H2,1-4H3 |
| PubChem CID | 3117 |
| 靶点 | Aldehyde Dehydrogenase (ALDH) |
| 通路 | Metabolic Enzyme&Protease |
| 背景说明 | Disulfiram是特异性的乙醛脱氢酶1型抗体 (ALDH1) 抑制剂。 |
| 生物活性 | Disulfiram (Tetraethylthiuram disulfide) is a specific inhibitor of aldehyde-dehydrogenase (ALDH1), used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells[1-5]. |
| 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 CuCl2 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]. |
| 细胞实验 | 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]. |
| 细胞实验 | The effect of disulfiram(0.15-5.0 μM)or sodium diethyldithiocarbamate(1.0 μM)on proliferation of malignant cell lines is studied in cultures stimulated with 10% FBS. Cell numbers are quantitated 24 to 72 hours later，as outlined below. In some experiments，disulfiram is added immediately after cells are plated. In other experiments，cells are plated and allowed to grow for 24 to 72 hours before fresh medium with disulfiram is added and cell numbers are assayed 24 to 72 hours later. Synergy is studied between disulfiram and N，N′-bis(2-chloroethyl-N-nitrosourea(carmustine，1.0-1，000 μM)or cisplatin(0.1-100 μg/mL)added to medium. The effect of metal ions on disulfiram is studied with 0.2 to 10 μM Cu2+(provided as CuSO4)，Zn2+(as ZnCl2)，Ag+(as silver lactate)，or Au3+(as HAuCl4·3H2O)ions added to growth medium，buffered to physiologic pH. To provide a biologically relevant source of copper，medium is supplemented with human ceruloplasmin at doses replicating low and high normal adult serum concentrations(250 and 500 mg/mL).[4] |
| 动物实验 | Adult female CB17-SCID mice are housed in a protected laminar flow facility with access to water and either a standard diet containing 87 ppm zinc or a zinc-supplemented diet containing 1，000 ppm Zn2+ as zinc acetate. Mice are injected s.c. in the right groin with 5×106 cells from a highly aggressive malignant melanoma obtained from a Carolinas Medical Center patient. The frozen tumor is passaged twice in SCID mice to adapt it to in vivo growth before use in these experiments. On the day of tumor injection，all mice began daily administration of drug. Drug is given in a total volume of 0.2 mL by gastric gavage via smooth Teflon-tipped needles inserted transorally into the stomach. Four groups are studied: tumor control(n=10; 0.2 mL olive oil daily; zinc diet of 87 ppm); zinc-supplemented control(n=10; 0.2 mL olive oil daily; zinc diet of 1，000 ppm); disulfiram(n=10; 200 mg/kg/d disulfiram in 0.2 mL olive oil; zinc diet of 87 ppm); and zinc-supplemented diet + disulfiram(n=10; 200 mg/kg/d disulfiram in 0.2 mL olive oil; zinc diet of 1，000 ppm). Mice are examined daily，the tumor is measured in two dimensions，and the tumor volume is estimated using the formula for an elipse. When estimated tumor volume approached 500 mm3 within any animal，all mice are euthanized. Tumors are excised，weighed，fixed in formalin，sectioned，and stained or immunostained for factor VIII. Slides are coded and examined by a blinded observer who identified vessels as deposits of red cells. For each slide，the number of vessels is counted in four different fields representative of the tumor. The average number of vessels per field is averaged per biopsy specimen and used to evaluate tumor vascularity.[1] |
| 数据来源文献 | [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. |
| 单位 | 瓶 |
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文献和实验【本资料源自公开渠道，如需（此处）屏蔽，请联系删除】
标题:Disulfiram-loaded copper sulfide nanoparticles for potential anti-glioma therapy
成员:Qing-Hua Lan, Chu-Chu Du, Run-Jie Yu, Jiaoyuan Zhai, Yannan Shi, Longfa Kou, Jian Xiao, Cui-Tao Lu, Ying-Zheng Zhao, Qing Yao
论文因子:5.875 发表期刊:INTERNATIONAL JOURNAL OF PHARMACEUTICS pmid:34371152
【本资料源自公开渠道，如需（此处）屏蔽，请联系删除】
标题:An Intrinsically Nontrimerizing Peptide Probe for Specifically Targeting Pathological Collagen in Connective Tissues
成员:Cai Xiangdong;Wei Wenyu;Bi Yihui; Liu Zhao;Bai Zh
论文因子:17.093 发表期刊:Advanced Functional Materials
1. 前目 叶绿体是绿色植物组织中一种重要的器官，其主要功能是执行光合作用。除此之外 ，许多重要的化合物也在叶绿体内合成，如植物激素、脂肪酸和油脂、氨基酸、维生素、嘌呤、嘧啶核酸、四吡咯类化合物及类异戊二烯等。叶绿体也是植物细胞内同化氮和硫的场所 [1] 。其内包含有大量的蛋白质结合伴侣、定位元件、辅因子伴侣、组装元件、肽酶及蛋白酶等，对于蛋白质生物合成和胞内平衡具有重要作用。叶绿体内的蛋白质种类多样，包括与质体 DNA 及 mRNA 结合的蛋白质，这些蛋白质对叶绿体内基因的表达具有重要
磷酰胺（DEPC) (Sigma) 、30% 甘油及蛋白酶抑制剂 [ 含有 1 μg/ml 抑肽酶（aprotinin) 、1 μg/ml 胃蛋白酶抑制剂（pepstatin) 、1 μg/ml 亮抑酶肽（leupeptin) 、0.1 mmol/L PMSF ] ，所有药品都来自于 Sigma ( 见注释 1 和注释 2) 。注意：媒介中的两种成分—— DEPC 和 β-巯基乙醇是有毒的，需要在通风橱中进行准备，并需要戴化学防护手套。 2.2 细胞核的提纯 ( 1 ) 样品
, we may find much more references regarding this issue. http://books.google.com/books?id=3mgPzNFjcWAC&pg=PA51&lpg=PA51&dq=gsk+tyrosine+phosphorylation+and+activity&source=bl&ots=x5ueTldpez&sig=CqRFJleXtEBn9OfelhODPAc28xs&hl=en&ei=KerNSu-XGcem8Abm-qmABA&sa=X&oi=book_result&ct
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