Auranofin

Auranofin

Catalog Number:
L002372569APE
Mfr. No.:
APE-B7687
Price:
$209
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      • Overview
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          Background

          Auranofin is inhibitor of thioredoxin reductase (TrxR) with IC50 value of ∼ 88 nM [1].
          TrxR, a ubiquitous homodimeric flavoenzyme, functions by transferring reducing equivalents from NADPH to thioredoxin. It has been suggested to play roles in diverse physiological and pathological conditions such as apoptosis, cancer, parasitoses, chronic inflammatory and autoimmune diseases, as well as neurodegenerative disorders [2].
          In Helicobacter pylori (H. pylori), Auranofin completely inhibited bacterial growth at the concentration of 1.2 μM. Purified H. pylori TrxR was inhibited by Auranofin in a cell-free assay (IC50: ∼ 88 nM) [1]. In addition, in another study using murine 4T1 and EMT6 tumor cells, Auranofin potently radiosensitized tumor cells at concentrations of 3 ~ 10 μM [3].
          In 4T1 tumor-bearing mice, Auranofin combined with Buthionine Sulfoximine (BSO), subcutaneously administrated at the concentrations of 3 and 25 mg/kg, respectively, enhanced tumor radioresponse, resulting in a tumor growth delay of 13 days, and thereby significantly increased the medium survival rate, while neither of these pharmaceuticals were effective when administered on their own [3].

          [1]. Owings J P, McNair N N, Mui Y F, et al. Auranofin and N-heterocyclic carbene gold-analogs are potent inhibitors of the bacteria Helicobacter pylori. FEMS Microbiology Letters, 2016, 363(14): 1-6.
          [2]. Saccoccia F, Angelucci F, Boumis G, et al. Thioredoxin reductase and its inhibitors. Current Protein & Peptide Science, 2014, 15(6): 621-646.
          [3]. Wang H, Bouzakoura S, de Mey S, et al. Auranofin radiosensitizes tumor cells through targeting thioredoxin reductase and resulting overproduction of reactive oxygen species. Oncotarget, 2017, 8(22): 35728-35742.

      • Properties
        • CAS Number
          34031-32-8
          Molecular Formula
          C20H34AuO9PS
          Molecular Weight
          678.48
          Appearance
          A solid
          Purity
          98.00%
          Solubility
          ≥67.8 mg/mL in DMSO; insoluble in H2O; ≥31.6 mg/mL in EtOH
          Storage
          Store at RT

          * For Research Use Only

      • Reference
        • 1. Wang H, Zhang S, et al. "Synergistic lethality between PARP-trapping and alantolactone-induced oxidative DNA damage in homologous recombination-proficient cancer cells." Oncogene. 2020;10.1038/s41388-020-1191-x. PMID:32029902

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