217798-39-5
Chemical Structure
Ethaselen
Synonym(s): BBSKE
- CAS No.: 217798-39-5
- Formula:C16H12N2O2Se2
- Molecular Weight:422.20
IUPAC Name: 2,2'-(ethane-1,2-diyl)bis(benzo[d][1,2]selenazol-3(2H)-one)
InChIKey: SFFSGPCYJCMDJM-UHFFFAOYSA-N
SMILES: O=C1N([Se]C2=CC=CC=C12)CCN3[Se]C4=CC=CC=C4C3=O
Biological Activity: 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].
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Ethaselen | 98.0% | 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. | ||||||||||||||||||||
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- [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. [Content Brief]
- [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. [Content Brief]
Keywords
