Bioactivity | Aurothioglucose (Gold thioglucose), containing monovalent gold ion, is a potent active-site inhibitor of TrxR1 (thioredoxin reductase 1), with an IC50 of 65 nM. Aurothioglucose inhibits the DNA binding of NF-κB in vitro. Aurothioglucose shows anti-HIV and anti-rheumatic activities[1][2]. | ||||||||||||
Target | IC50: 65 nM (TrxR1) | ||||||||||||
Invitro | 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 with Ebselen (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: | ||||||||||||
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: | ||||||||||||
Name | Aurothioglucose | ||||||||||||
CAS | 12192-57-3 | ||||||||||||
Formula | C6H11AuO5S | ||||||||||||
Molar Mass | 392.18 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [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. [3]. Britt RD Jr, et al. The thioredoxin reductase-1 inhibitor aurothioglucose attenuates lung injury and improves survival in a murine model of acute respiratory distress syndrome. Antioxid Redox Signal. 2014 Jun 10;20(17):2681-91. [4]. Naruta E, et al. Hypolipidemic effect of pantothenic acid derivatives in mice with hypothalamic obesity induced by aurothioglucose. Exp Toxicol Pathol. 2001 Oct;53(5):393-8. |