Ethaselen (BBSKE) is an orally active, selective thioredoxin reductase ( TrxR ) inhibitor with IC 50 s of 0.5 and 0.35 μM for the wild-type human TrxR1 and rat TrxR1 , respectively. Ethaselen specifically binds to the unique selenocysteine-cysteine redox pair in the C-terminal active site of mammalian TrxR1 . Ethaselen, an organoselenium compound, is a potent antitumor candidate that exerts potent inhibition on non-small cell lung cancer (NSCLC) by targeting TrxR .
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