Auranofin

产品编号: T1303 别名:

醋硫葡金,SKF-39162

Auranofin是硫氧还蛋白还原酶抑制剂，IC50为0.2 μM。它也是一种抗风湿剂，用于治疗类风湿性关节炎，改善关节炎症状。

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CAS：34031-32-8

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生物活性化学信息储存和溶解度信息参考文献引用文献

产品描述

Auranofin is an antirheumatic agent, is used to treat rheumatoid arthritis, improves arthritis symptoms including painful or tender and swollen joints and morning stiffness.

体外活性

Auranofin is a drug that is approved for the treatment of rheumatoid arthritis but is being investigated for potential therapeutic application in many other diseases including cancer, neurodegenerative disorders. Auranofin induces apoptosis in cells through a Bax/Bak-dependent mechanism associated with selective disruption of mitochondrial redox homeostasis in conjunction with oxidation of Prx3[1]. Auranofin inhibits proliferation and survival of SKOV3 cells in a dose- and time-dependent manner. Auranofin treatment activates the pro-apoptotic caspase-3, increases protein levels of apoptosis-inducing proteins Bax and Bim and reduces the expression of the anti-apoptotic mediator Bcl-2 in SKOV3 cells[2]. Auranofin is a lipophilic gold compound with anti-inflammatory and immunosuppressive properties. Auranofin inhibits the cell growth and induction of mitochondrial apoptosis in PC3 human prostate cancer cells. Treatment with auranofin significantly inhibits cell viability with an IC50 value of 2.5 μM after 24 h[3].

体内活性

Prophylactic treatment of adjuvant-induced arthritis rats with auranofin results in a slight reduction in paw edema, a complete normalization of the depressed IL-2 production, and a reduction of the elevated IL-1 production, without effect on the depressed IL-3 production[4].

细胞实验

Auranofin is dissolved in DMSO. Cells are treated with auranofin (0, 50, 100, 200 and 400 nM) for 72 h for the dose-dependent response assay and 100 nM of auranofin is added into the wells for 0, 24, 72 and 120 h for the time-dependent response assay. Control cultures are treated with DMSO. Cell viability is measured by the MTT assay[2].

Cas No.

34031-32-8

分子式

C20H34AuO9PS

分子量

678.48

别名

醋硫葡金;SKF-39162;Auranofin

参考文献

[1]Lu H, Lu W, Zhu Y, et al. Auranofin Has Advantages over First-Line Drugs in the Treatment of Severe Streptococcus suis Infections[J]. Antibiotics. 2021, 10(1): 26.[2]Zhang Y, Zhou J, Ye Q, et al. 6-Dithio-2′-deoxyguanosine analogs induce reactive oxygen species-mediated tumor cell apoptosis via bi-targeting thioredoxin 1 and telomerase[J]. Toxicology and Applied Pharmacology. 2020: 115079.[3]Park N, et al. Auranofin promotes mitochondrial apoptosis by inducing annexin A5 expression and translocation in human prostate cancer cells. J Toxicol Environ Health A. 2014;77(22-24):1467-76.[4]Cox AG, et al. The thioredoxin reductase inhibitor auranofin triggers apoptosis through a Bax/Bak-dependent process that involves peroxiredoxin 3 oxidation. Biochem Pharmacol. 2008 Oct 30;76(9):1097-109.[5]Lee JC, et al. Effect of auranofin treatment on aberrant splenic interleukin production in adjuvant arthritic rats. J Immunol. 1987 Nov 15;139(10):3268-74.[6]Zheng X, Yang Z, Gu Q, et al. The protease activity of human ATG4B is regulated by reversible oxidative modification[J]. Autophagy. 2019 (just-accepted).[7]Xia Y, Chen J, Yu Y, et al. Compensatory combination of mTOR and TrxR inhibitors to cause oxidative stress and regression of tumors[J]. Theranostics. 2021, 11(9): 4335.[8]Park SH, et al. Auranofin displays anticancer activity against ovarian cancer cells through FOXO3 activation independent of p53. Int J Oncol. 2014 Oct;45(4):1691-8.

引用文献

[1]Zheng X, Yang Z, Gu Q, et al. The protease activity of human ATG4B is regulated by reversible oxidative modification. Autophagy. 2019 [2]Xia Y, Chen J, Yu Y, et al. Compensatory combination of mTOR and TrxR inhibitors to cause oxidative stress and regression of tumors. Theranostics. 2021, 11(9): 4335.[3]Lu H, Lu W, Zhu Y, et al. Auranofin Has Advantages over First-Line Drugs in the Treatment of Severe Streptococcus suis Infections. Antibiotics. 2021, 10(1): 26.[4]Zhang Y, Zhou J, Ye Q, et al. 6-Dithio-2′-deoxyguanosine analogs induce reactive oxygen species-mediated tumor cell apoptosis via bi-targeting thioredoxin 1 and telomerase. Toxicology and Applied Pharmacology. 2020: 115079

储存和溶解度

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years

剂量换算 Auranofin 34031-32-8

对于各种应用，安全且有效的用药剂量是很有必要的了解更多

体内实验配液计算器

第一步：请输入动物实验的基本信息

剂量 mg/kg

每只动物体重 g

给药体积 ul

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO +

% +

% Tween 80 +

% ddH₂O

% DMSO +

重置计算

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

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已知质量的化合物在一定体积内形成的溶液的浓度

质量

浓度

体积

分子量

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制备已知体积和浓度溶液所需的化合物质量
将已知质量的化合物溶解到所需浓度所需的溶液体积
已知质量的化合物在一定体积内形成的溶液的浓度

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体积（起始）

浓度（终点）

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分子结构式

总分子量

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技术支持

在抑制剂处理说明中可以找到您可能遇到的问题的答案。主题包括如何准备储备溶液，如何存储产品以及基于细胞的测定和动物实验需要特别注意的问题。

Keywords

SARS coronavirus 醋硫葡金 Auranofin SKF-39162 SKF 39162 inhibit Bacterial Inhibitor SKF39162 SARS-CoV 34031-32-8

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Auranofin

醋硫葡金,SKF-39162

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