Aurothioglucose (Gold thioglucose) 含有单价金离子,是一种有效的 TrxR1 (硫氧还蛋白还原酶 1) 的活性位点抑制剂,其 IC50 为 65 nM。Aurothioglucose 在体外抑制 NF-κB 的 DNA 结合。Aurothioglucose 具有抗 HIV 和抗风湿的活性。
生物活性
Aurothioglucose (Gold thioglucose), containing monovalent gold ion, is a potent active-site inhibitor of TrxR1 (thioredoxin reductase 1), with an IC 50 of 65 nM. Aurothioglucose inhibits the DNA binding of NF-κB in vitro. Aurothioglucose shows anti-HIV and anti-rheumatic activities.
性状
Solid
IC50 & Target[1][2]
IC50: 65 nM (TrxR1)
体外研究(In Vitro)
Aurothioglucose (0-100 μM, 24-72 h) inhibits TrxR1 activity in HeLa cell cytosol but has no effect on the viability of the cells. Aurothioglucose (0-30 μM, 6 h) exhibits very low cytotoxicity on cells.Aurothioglucose (0-20 μM, 24 h) combined with Ebselen (HY-13750) shows a strong synergistic effect, leading to Trx1 (thioredoxin 1) oxidation, reactive oxygen species (ROS) accumulation, and cell death.Aurothioglucose (0-100 μM, 3-12 days) inhibits p24 levels in OM10.1 and Ach2 cells, and inhibits HIV-1 replication in vitro.Aurothioglucose (0-25 μM, 12 days) increases the accumulation of metal gold in a dose-dependent manner. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Aurothioglucose (25 mg/kg, i.p., single) significantly attenuates lung injury and enhances survival in a clinically relevant murine model of ARDS. The protective effects of Aurothioglucose are GSH dependent.
Aurothioglucose (300 mg/kg, i.p., single) induces hypothalamic obesity in mice. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Du Y, et al. Glutathione and glutaredoxin act as a backup of human thioredoxin reductase 1 to reduce thioredoxin 1 preventing cell death by aurothioglucose. J Biol Chem. 2012 Nov 2;287(45):38210-9. [2]. Traber KE, et al. Anti-rheumatic compound aurothioglucose inhibits tumor necrosis factor-alpha-induced HIV-1 replication in latently infected OM10.1 and Ach2 cells. Int Immunol. 1999 Feb;11(2):143-50.
溶解度数据
In Vitro: H2O : 125 mg/mL (318.73 mM; Need ultrasonic)DMSO : 6 mg/mL (15.30 mM; Need ultrasonic)配制储备液