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 ofTrxR1(thioredoxin reductase 1), with anIC50of 65 nM. Aurothioglucose inhibits the DNA binding ofNF-κBin vitro. Aurothioglucose shows anti-HIV and anti-rheumatic activities[1][2]. |
| IC50& Target | |
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[1].
Aurothioglucose (0-30 μM, 6 h) exhibits very low cytotoxicity on cells[1].
Aurothioglucose (0-20 μM, 24 h) combined withEbselen(HY-13750) shows a strong synergistic effect, leading to Trx1 (thioredoxin 1) oxidation, reactive oxygen species (ROS) accumulation, and cell death[1].
Aurothioglucose (0-100 μM, 3-12 days) inhibits p24 levels in OM10.1 and Ach2 cells, and inhibits HIV-1 replication in vitro[2].
Aurothioglucose (0-25 μM, 12 days) increases the accumulation of metal gold in a dose-dependent manner[2].
Cell Viability Assay[1] | Cell Line: | HeLa cells | | Concentration: | 0, 5, 10, 50, 100 μM | | Incubation Time: | 24, 48, 72 h | | Result: | Inhibited TrxR activity by more than 90% at 100 μM in HeLa cells. Cell viability was unaffected by ATG treatment, even at 100 μM after 72 h. |
Western Blot Analysis[1] | Cell Line: | HeLa cells | | Concentration: | 0, 5, 10, and 100 μM | | Incubation Time: | 24 h | | Result: | Showed no significant oxidation of Trx1 or Trx2 in HeLa cells. |
Western Blot Analysis[2] | Cell Line: | OM10.1, Ach2 cells | | Concentration: | 0, 4, 10, 25 and 100 μM | | Incubation Time: | 3, 6 or 12 days | | Result: | Significantly inhibited p24 levels. After 12 days of incubation, the viability of cells treated with 10, 25 and 100 μM Aurothioglucose had decreased to 60% of the control. |
|
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[3].
Aurothioglucose (300 mg/kg, i.p., single) induces hypothalamic obesity in mice[4].
| Animal Model: | Adult male C3H/HeN mice (8-12 week, LPS/hyperoxia-exposed mice, inflammation/hyperoxia ARDS model)[3] | | Dosage: | 25 mg/kg | | Administration: | IP, single, at 12 h after intratracheal LPS administration | | Result: | Significantly attenuated lung injury, increased lung GCLM expression and GSH levels, and decreased mortality. |
|
| 分子量 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 中文名称 | |
| 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 | | In solvent | -80°C | 6 months | | -20°C | 1 month |
|
| 溶解性数据 | 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 | 1 mM | 2.5498 mL | 12.7492 mL | 25.4985 mL | | 5 mM | 0.5100 mL | 2.5498 mL | 5.0997 mL | | 10 mM | 0.2550 mL | 1.2749 mL | 2.5498 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
m.cnreagent.com