Auranofin

Biological Activity

Auranofin is an inhibitor of thioredoxin reductase (TrxR) (IC₅₀ = 20 nM; K_i = 4 nM for the NADPH-reduced form of human cytosolic TrxR). Thought to induce the mitochondrial permeability transition via inhibition of mitochondrial TrxR. Also exhibits anti-inflammatory and immunosuppressive activities; inhibits 5-lipoxygenase at high concentrations and stimulates LTA hydrolase at low concentrations. Also inhibits SARS-CoV-2 infection in Huh7 cell line (IC₅₀ = 1.4 μM)

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Auranofin blocks interleukin-6 signalling by inhibiting phosphorylation of JAK1 and STAT3.
   Kim et al.
   Immunology, 2007;122:607
2. Induction of mitochondrial permeability transition by auranofin, a gold(I)-phosphine derivative.
   Rigobello et al.
   Br.J.Pharmacol., 2002;136:1162
3. Human placenta thioredoxin reductase. Isolation of the selenoenzyme, steady state kinetics, and inhibition by therapeutic gold compounds.
   Gromer et al.
   J.Biol.Chem., 1998;273:20096
4. Auranofin stimulates LTA hydrolase and inhibits 5-lipoxygenase/LTA synthase activity of isolated human neutrophils.
   Betts et al.
   Biochem.Pharmacol., 1990;39:1233
5. The FDA-approved gold drug auranofin inhibits novel coronavirus (SARS-COV-2) replication and attenuates inflammation in human cells.
   Rothan et al.
   Virology, 2020;547:7

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