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二硫化四乙基秋兰姆(TETD), 醛脱氢酶抑制剂

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货号 (SKU) 包装规格 是否现货 价格 数量
D408480-1ml
1ml 现货 Stock Image
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Compound libraries (12333)

基本描述

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。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 抑制剂
作用机制 醛脱氢酶抑制剂
产品介绍

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%

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)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
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)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
FBP1 Tchem 果糖-1,6-双磷酸酶 1(Fructose-1,6-bisphosphatase 1) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
CYP2C9 Tchem 细胞色素 P450 2C9(Cytochrome P450 2C9) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
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)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
MGLL Tchem 单甘油酯脂肪酶(Monoglyceride lipase) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
LOXL2 Tchem 赖氨酰氧化酶同源物 2(Lysyl oxidase homolog 2) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
LOXL3 Tchem 赖氨酰氧化酶同源物 3(Lysyl oxidase homolog 3) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
LOX Tchem 蛋白质赖氨酸6-氧化酶(Protein-lysine 6-oxidase) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
LOXL4 Tchem 赖氨酰氧化酶同源物 4(Lysyl oxidase homolog 4) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
ALDH1A1 Tchem 视网膜脱氢酶1(Retinal dehydrogenase 1) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
ALDH2 Tclin 乙醛脱氢酶,线粒体(Aldehyde dehydrogenase, mitochondrial) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
GSDMD Tchem 加德明-D(Gasdermin-D) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

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=

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)

象形图 GHS08,   GHS09,   GHS07
信号词 Warning
危险声明

H373: 通过长时间或反复暴露对器官造成损害

H302: 吞食有害

H317: 可能引起皮肤过敏反应

H400: 对水生生物有剧毒

H410: 对水生生物有剧毒并具有长期持续影响

预防措施声明

P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾

P273: 避免释放到环境中。

P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。

P302+P352: 如皮肤沾染:用水充分清洗。

P321: 特殊处理(请参阅此标签上的...)。

P501: 将内容物/容器处理到。。。

P264: 处理后要彻底洗手。

P260: 不要吸入灰尘/烟雾/气体/雾/蒸汽/喷雾。

P270: 使用本产品时,请勿进食、饮水或吸烟。

P272: 被污染的工作服不允许离开工作场所

P333+P313: 如发生皮肤刺激或皮疹:求医/就诊。

P362+P364: 脱掉沾污的衣服,清洗后方可重新使用。

P391: 收集溢出物

P330: 漱口

P301+P317: 如果被吞咽:请寻求医疗帮助。

P319: 如果你感到不适,请寻求医疗帮助。

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:

溶液计算器