Ethaselen (Synonyms: BBSKE) |
رقم الكتالوجGC63488 |
Ethaselen (BBSKE) هو مثبط اختزال ثيوردوكسين انتقائي نشط عن طريق الفم (TrxR) مع IC50s من 0.5 و 0.35 ميكرومتر للإنسان من النوع البري TrxR1 و الفئران TrxR1 ، على التوالييرتبط Ethaselen على وجه التحديد بزوج الأكسدة والاختزال السيلينوسيستين الفريد في الموقع النشط للطرف C للثدييات TrxR1Ethaselen ، مركب السيلينيوم العضوي ، هو مرشح قوي مضاد للأورام يمارس تثبيطًا قويًا على سرطان الرئة ذو الخلايا غير الصغيرة (NSCLC) عن طريق استهداف TrxR
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 217798-39-5
Sample solution is provided at 25 µL, 10mM.
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].
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].
Ethaselen(BBSKE; 36-108 mg/kg/day; PO; for 10 days) shows increased inhibition of tumor growth in a dose-independent manner[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.
[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.
Average Rating: 5
(Based on Reviews and 36 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *