计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 24 篇同行评审文献引用。
概述
Disulfiram is a DNA demethylating agent and DIG1 inducer which inhibits prostate cancer cell growth by inhibition of DNA methyltransferase (Dnmt). In addition, studies indicate that disulfiram inhibits aldehyde dehydrogenase (ALDH) resulting in the accumulation of acetaldehyde upon ethanol ingestion. Alternate studies show that disulfiram also inhibits dopamine β-hydroxylase (DBH), an enzyme important in converting dopamine to norepinephrine in noradrenergic neurons. Futhermore, disulfiram can reduce toxicity and carcinogenesis by inhibiting the cytochrome P450IIE1 (CYP2E1). It has been reported that disulfiram can also inhibit tumor cell growth via binding to cellular copper, which inhibits proteosome activity and induces apoptosis. Disulfiram is an inhibitor of ADH and V-ATPase醇脱氢酶抑制剂。 An ALDH and tumor cell growth inhibitor
Information
Disulfiram (NSC 190940, Tetraethylthiuram disulfide, TETD) is a specific inhibitor ofaldehyde-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
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]
Cell Data
cell lines：
Concentrations：
Incubation Time：
Powder Purity:≥98%
规格
英文别名
Tetraethylthiuram disulfide, TETD | N,N,N',N'-tetraethyl-thioperoxydicarbonic diamide([(H2N)C(S)]2S2)
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Disulfiram (NSC 190940)
生化机理
双硫仑（NSC 190940，二硫化四乙基秋兰姆，TETD）是醛脱氢酶（ALDH）的特异性抑制剂，对 hALDH1 和 hALDH2 的 IC50 分别为 0.15 μM 和 1.45 μM。双硫仑通过产生对酒精的急性敏感性来治疗慢性酒精中毒。双硫仑可诱导细胞凋亡。二硫仑也是气敏素 D（GSDMD）形成孔隙的抑制剂。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
醛脱氢酶抑制剂
名称和识别符
EC号
202-607-8
分子类型
小分子
Isomeric SMILES
CCN(CC)C(=S)SSC(=S)N(CC)CC
分子量
296.54
Beilstein号
1712560
Reaxy-Rn
1712560
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=1712560&ln=
技术文档
高级数据
产品属性
| ALogP | 3.9 |
|---|
关联靶点（人）
CYP2C19
Tchem
细胞色素 P450 2C19(Cytochrome P450 2C19)
(1 活性数据)
EHMT2
Tchem
组蛋白赖氨酸N-甲基转移酶EHMT2(Histone-lysine N-methyltransferase EHMT2)
(1 活性数据)
FBP1
Tchem
果糖-1,6-双磷酸酶 1(Fructose-1,6-bisphosphatase 1)
(1 活性数据)
CYP2C9
Tchem
细胞色素 P450 2C9(Cytochrome P450 2C9)
(1 活性数据)
TRPA1
Tclin
瞬时受体电位阳离子通道亚家族A成员1(Transient receptor potential cation channel subfamily A member 1)
(1 活性数据)
MGLL
Tchem
单甘油酯脂肪酶(Monoglyceride lipase)
(1 活性数据)
LOXL2
Tchem
赖氨酰氧化酶同源物 2(Lysyl oxidase homolog 2)
(1 活性数据)
LOXL3
Tchem
赖氨酰氧化酶同源物 3(Lysyl oxidase homolog 3)
(1 活性数据)
LOX
Tchem
蛋白质赖氨酸6-氧化酶(Protein-lysine 6-oxidase)
(1 活性数据)
LOXL4
Tchem
赖氨酰氧化酶同源物 4(Lysyl oxidase homolog 4)
(1 活性数据)
ALDH1A1
Tchem
视网膜脱氢酶1(Retinal dehydrogenase 1)
(1 活性数据)
ALDH2
Tclin
乙醛脱氢酶，线粒体(Aldehyde dehydrogenase, mitochondrial)
(1 活性数据)
GSDMD
Tchem
加德明-D(Gasdermin-D)
(1 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 26 mg/mL (201.37 mM); Water: 26 mg/mL (201.37 mM); Ethanol: 26 mg/mL (201.37 mM);
熔点
69-71°C
安全和危险性（GHS）
WGK Germany
3
RTECS
JO1225000
Merck Index
3364
个人防护装备
dust mask type N95 (US),Eyeshields,Faceshields,Gloves
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
通过匹配包装上的批号来查找并下载产品的 COA，每批产品都进行了严格的验证，您可放心使用！
| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
 L2214637 |
分析证书 | D408480 |
技术文档和文章
Inflammatory Signaling Pathway Research Guide: Danger Signal Recognition, Core Signaling Modules, Detection Readouts, and Representative Research Reagents
目录： 技术文章
此产品的引用文献
溶液计算器
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