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Ethaselen (Synonyms: BBSKE)

Cat. No.: HY-116749
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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.

For research use only. We do not sell to patients.

Ethaselen Chemical Structure

Ethaselen Chemical Structure

CAS No. : 217798-39-5

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Description

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].

IC50 & Target

TrxR[1]

In Vitro

Ethaselen (2.5-10 μM; 12, 24 hours) suppresses A549 cell viability in a both concentration- and time-dependent manner. H1666, which has considerably lower TrxR1 expression level, is less susceptible to 24 h treatment with Ethaselen[1].
Ethaselen inhibits the intracellular TrxR1 activity in a concentration- and time-dependent manner, with IC50 values of 4.2 and 2 μM for 12- and 24-h treatments, respectively[1].
Ethaselen (2.5-10 μM; 12, 24 hours) has no effect on the protein amounts of TrxR1 and Trx. The mRNA level of TrxR1 does not show significant alteration in Ethaselen-treated A549 cells[1].
Ethaselen (2.5-50 μM; 1-24 hours) causes intracellular Trx oxidation in A549 cells[1].
Ethaselen (5-10 μM; 12, 24 hours) causes a clear concentration-dependent increase in ROS levels in A549 cells[1].
The inhibition constants for Ethaselen binding to free enzyme (Ki) and the enzyme-substrate complex (Kis) were determined to be 0.022 and 0.087 μM, respectively. Ethaselen also inhibits mammalian TrxR1 in a time-dependent manner possibly by forming a covalent Se-S bond with Cys497 of Trx[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: A549 cell
Concentration: 2.5, 5, 7.5, 10 μM
Incubation Time: 12, 24 hours
Result: Suppressed A549 cell viability in a both concentration- and time-dependent manner.
In Vivo

Ethaselen (BBSKE; 36-108 mg/kg/day; PO; for 10 days) shows increased inhibition of tumor growth in a dose-independent manner[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Five-week-old female BALB/c nude mice with A549 cell[2]
Dosage: 36, 72, 108 mg/kg
Administration: PO; daily; for 10 days
Result: Showed increased inhibition of tumor growth, and the inhibition levels increased with the dose.
The TrxR activity levels of the high dose group (108 mg/kg) decreased more than the middle dose group (72 mg/kg) and low dose group (36 mg/kg).
Molecular Weight

422.20

Formula

C₁₆H₁₂N₂O₂Se₂

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