217798-39-5

Ethaselen (BBSKE) is an orally active, selective thioredoxin reductase (TrxR) inhibitor with IC50s 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[1][2].

[1] Lihui Wang, et al. Ethaselen: a potent mammalian thioredoxin reductase 1 inhibitor and novel organoselenium anticancer agent. Free Radic Biol Med. 2012 Mar 1;52(5):898-908. DOI:10.1016/j.freeradbiomed.2011.11.034
[2] Suo-Fu Ye, et al. Dose-biomarker-response modeling of the anticancer effect of ethaselen in a human non-small cell lung cancer xenograft mouse model. Acta Pharmacol Sin. 2017 Feb;38(2):223-232. DOI:10.1038/aps.2016.114