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Ethaselen

Catalog No. T39664 CAS 217798-39-5

Synonyms: BBSKE

Ethaselen (BBSKE), a selective thioredoxin reductase (TrxR) inhibitor, is orally active with IC50s of 0.5 and 0.35 μM for wild-type human TrxR1 and rat TrxR1, respectively. Ethaselen specifically binds to the unique selenocysteine-cysteine redox pair located in the C-terminal active site of mammalian TrxR1. As an organoselenium compound, it demonstrates potent antitumor activity against non-small cell lung cancer (NSCLC) by targeting TrxR.

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Ethaselen, CAS 217798-39-5

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Purity: 97.58%

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Description	Ethaselen (BBSKE), a selective thioredoxin reductase (TrxR) inhibitor, is orally active with IC50s of 0.5 and 0.35 μM for wild-type human TrxR1 and rat TrxR1, respectively. Ethaselen specifically binds to the unique selenocysteine-cysteine redox pair located in the C-terminal active site of mammalian TrxR1. As an organoselenium compound, it demonstrates potent antitumor activity against non-small cell lung cancer (NSCLC) by targeting TrxR.
In vitro	Ethaselen (2.5-10 μM; 12, 24 hours) diminishes the viability of A549 cells in both a concentration- and time-dependent fashion. H1666 cells, which exhibit a significantly lower expression level of TrxR1, display reduced sensitivity to Ethaselen after 24 hours of treatment[1]. Additionally, Ethaselen selectively inhibits TrxR1 activity within the cell, reflected by IC50 values of 4.2 and 2 μM for 12 and 24 hours of exposure, respectively, without altering the protein quantities of TrxR1 and Trx, nor the mRNA levels of TrxR1 in treated A549 cells[1]. Furthermore, treatment with Ethaselen (2.5-50 μM; 1-24 hours) leads to Trx oxidation, and a dosage of 5-10 μM (12, 24 hours) induces a notable increase in ROS levels in a dose-dependent manner in A549 cells[1]. The inhibition constants of Ethaselen for binding to the free enzyme (K_i) and the enzyme-substrate complex (K_is) are 0.022 and 0.087 μM, respectively, suggesting Ethaselen impedes mammalian TrxR1 by potentially forming a covalent bond with Cys497 of Trx in a time-dependent process[1]. A Cell Viability Assay confirmed Ethaselen’s effectiveness in suppressing A549 cell viability over 12 and 24 hours at concentrations ranging from 2.5 to 10 μM, further emphasizing its concentration and time dependency[1].
In vivo	Ethaselen (BBSKE; 36-108 mg/kg/day; PO; for 10 days) demonstrates a dose-independent enhancement in tumor growth inhibition in female BALB/c nude mice inoculated with A549 cells[2]. The study highlighted that with escalating doses, the extent of tumor suppression increased. Furthermore, the highest dosage group (108 mg/kg) exhibited a more significant decrement in TrxR activity compared to both the intermediate (72 mg/kg) and lowest dose groups (36 mg/kg), underscoring a dose-related efficacy in reducing TrxR activity levels.

Synonyms	BBSKE
Molecular Weight	422.226
Formula	C16H12N2O2Se2
CAS No.	217798-39-5

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Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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. 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.

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Ethaselen 217798-39-5 BBSKE inhibitor inhibit

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