Ethaselen

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Ethaselen

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

217798-39-5

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
25mg	电议
50mg	电议

产品介绍

Ethaselen (BBSKE) 是具有口服活性的，选择性的硫氧还蛋白还原酶 (TrxR) 抑制剂，对野生型人 TrxR1 和大鼠 TrxR1 的 IC50 分别为 0.5 和 0.35 μM。Ethaselen 特异性结合哺乳动物 TrxR1 C 端活性位点中独特的硒代半胱氨酸-半胱氨酸氧化还原对。Ethaselen 是一种有机硒化合物，一种有效的抗肿瘤候选药物，可通过靶向 TrxR 对非小细胞肺癌 (NSCLC) 发挥有效抑制作用。

Cas No.	217798-39-5
别名	BBSKE
分子式	C₁₆H₁₂N₂O₂Se₂
分子量	422.2
溶解度	DMSO : 12.5 mg/mL (29.61 mM; ultrasonic and warming and heat to 60°C)
储存条件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	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.