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Metabolism
Dehydrogenase inhibitor
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COVID-19 inhibitor
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Apoptosis related activator
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Pyroptosis inhibitor
Disulfiram
僅限科研使用
Disulfiram
別名: NSC 190940, Tetraethylthiuram disulfide, TETD 中文名稱：雙硫侖
Disulfiram是一個特異性的乙醛脫氫酶 aldehyde-dehydrogenase (ALDH) 抑制劑，對hALDH1和hALDH2的IC50值分別0.15 μM和1.45 μM。Disulfiram 可用于治療慢性酒精中毒，對酒精產(chǎn)生急性敏感性。Disulfiram 可誘導(dǎo)凋亡。Disulfiram 還是一種通過 gasdermin D (GSDMD) 作用的孔隙形成抑制劑。
Disulfiram Chemical Structure
CAS: 97-77-8
產(chǎn)品質(zhì)控
批次：
純度：
99.91%
99.91
Disulfiram相關(guān)產(chǎn)品
相關(guān)信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells expressing BCA2 and estrogen receptor after 72 hrs by MTT assay, IC50 = 0.1 μM. | 20222671 | |
| CHO | Function assay | 30 mins | Inhibition of recombinant human LOXL3 expressed in CHO cells using diaminopentane as substrate preincubated for 30 mins followed by substrate addition measured after 1 hr by fluorimetric method, IC50 = 0.093 μM. | 30098867 | |
| insect cells | Function assay | 30 mins | Inhibition of recombinant human LOXL4 expressed in baculovirus infected insect cells using diaminopentane as substrate preincubated for 30 mins followed by substrate addition measured after 1 hr by fluorimetric method, IC50 = 0.059 μM. | 30098867 | |
| NS0 | Function assay | 30 mins | Inhibition of recombinant LOXL2 (unknown origin) expressed in NS0 cells using diaminopentane as substrate preincubated for 30 mins followed by substrate addition measured after 1 hr by fluorimetric method, IC50 = 0.15 μM. | 30098867 | |
| T47D | Antiproliferative assay | 72 hrs | Antiproliferative activity against human T47D cells expressing BCA2 and estrogen receptor after 72 hrs by MTT assay, IC50 = 0.17 μM. | 20222671 | |
| MDA-MB-231 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MDA-MB-231 cells expressing BCA2 and ERalpha after 72 hrs by MTT assay, IC50 = 0.32 μM. | 20222671 | |
| HEK293 | Function assay | 30 mins | Inhibition of recombinant human LOX expressed in HEK293 cells using diaminopentane as substrate preincubated for 30 mins followed by substrate addition measured after 1 hr by fluorimetric method, IC50 = 0.32 μM. | 30098867 | |
| MCF10A | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF10A cells after 72 hrs by MTT assay, IC50 = 10 μM. | 20222671 | |
| HepG2 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 38 μM. | 29571571 | |
| CHO | Function assay | Agonist activity at human TRPA1 channel expressed in CHO cells assessed as increase in intracellular calcium levels, EC50 = 3 μM. | 20356305 | ||
| CEM-SS | Antiviral assay | Antiviral activity against HIV-1 in CEM-SS cells using XXT assay, IC50 = 3.9 μM. | 9207937 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 29435139 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| fibroblast cells | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 29435139 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | ||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 29435139 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Disulfiram是一個特異性的乙醛脫氫酶 aldehyde-dehydrogenase (ALDH) 抑制劑，對hALDH1和hALDH2的IC50值分別0.15 μM和1.45 μM。Disulfiram 可用于治療慢性酒精中毒，對酒精產(chǎn)生急性敏感性。Disulfiram 可誘導(dǎo)凋亡。Disulfiram 還是一種通過 gasdermin D (GSDMD) 作用的孔隙形成抑制劑。 | ||||
|---|---|---|---|---|---|
| 靶點 |
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| 體外研究(In Vitro) | ||||
| 體外研究活性 | 在乳腺癌細胞MDA-MB-231和MCF10DCIS.com細胞中，Disulfiram銅配合物誘在導(dǎo)凋亡的癌細胞死亡前有效抑制培養(yǎng)的蛋白酶體的活性，而不在正常的，永生化的MCF-10A細胞中發(fā)揮這樣的作用。[1] Disulfiram，在臨床上使用的抗酒精中毒的藥物，以劑量依賴性的方式強烈抑制組成和5-FU誘導(dǎo)的NF-κB活性。Disulfiram既抑制NF-κB的核轉(zhuǎn)位和DNA結(jié)合活性，但對5-FU誘導(dǎo)的IkappaBalpha降解沒有影響。在DLD-1和RKO（WT）細胞系中，Disulfiram顯著增強5-FU的凋亡作用并協(xié)同增強5-FU的細胞毒性。在5-FU的耐藥細胞系H630中，Disulfiram也有效地廢除5-FU化療效果。[2] Disulfiram降低活細胞的數(shù)量，加入氯化銅顯著增強DSF誘導(dǎo)的細胞死亡，比對照組低10％。[3] 在黑素瘤細胞中，與較低濃度Disulfiram相比，Disulfiram與銅離子和鋅離子聯(lián)用可降低細胞周期蛋白A的表達，并減少在體外增殖。[4] |
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|---|---|---|---|---|
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | Disulfiram顯著抑制腫瘤生長達74％，這和體內(nèi)蛋白酶抑制相關(guān)聯(lián)（通過減少的水平的腫瘤組織蛋白酶活性和泛素化的蛋白質(zhì)和天然蛋白酶底物的p27和Bax的積累的測量）。Disulfiram還誘導(dǎo)細胞凋亡（通過半胱天冬荷瘤小鼠的MDA-MB-231腫瘤異種移植物的活化和凋亡細胞核的形成）。[1] Disulfiram阻斷P-糖蛋白擠壓泵，抑制轉(zhuǎn)錄因子核因子-κB，使腫瘤對化療敏感，減少血管生成，并抑制小鼠腫瘤的生長。在黑色素瘤移植的嚴(yán)重聯(lián)合免疫缺陷小鼠中，Disulfiram抑制生長和血管生成，這些效果是通過鋅離子補充加強。[4] |
|
|---|---|---|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05626920 | Recruiting | Inherited Retinal Dystrophy Primarily Involving Sensory Retina |
University of Washington |
December 2023 | Phase 1|Phase 2 |
| NCT04485130 | Terminated | Covid19 |
University of California San Francisco |
August 18 2021 | Phase 2 |
| NCT03151772 | Terminated | Glioblastoma |
Sahlgrenska University Hospital Sweden |
January 29 2018 | Early Phase 1 |
| NCT02309801 | Completed | Healthy |
Parc de Salut Mar|Ministerio de Sanidad Servicios Sociales e Igualdad |
July 2012 | Phase 1 |
化學(xué)信息&溶解度
| 分子量 | 296.54 | 分子式 | C10H20N2S4 |
| CAS號 | 97-77-8 | SDF | Download Disulfiram SDF |
| Smiles | CCN(CC)C(=S)SSC(=S)N(CC)CC | ||
| 儲存條件(自收到貨起) | |||
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體外溶解度 |
DMSO : 59 mg/mL ( (198.96 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Ethanol : 59 mg/mL (198.96 mM) Water : Insoluble |
摩爾濃度計算器 |
|
體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | ||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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