| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| E656849-1ml |
1ml |
期货  |
|
| 别名 | 乙烷硒啉 |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | Ethaselen |
| 生化机理 | Ethaselen (BBSKE) 是一种口服活性选择性硫氧还原酶（TrxR）抑制剂，对野生型人类 TrxR1 和大鼠 TrxR1 的 IC 50 s 分别为 0.5 和 0.35 μM。Ethaselen 能特异性地与独特的硒半胱氨酸-半胱氨酸氧化还原酶结合。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 产品介绍 |
Ethaselen (BBSKE) is an orally active, selective thioredoxin reductase (TrxR) inhibitor with IC 50 s 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 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. Ethaselen inhibits the intracellular TrxR1 activity in a concentration- and time-dependent manner, with IC 50 values of 4.2 and 2 μM for 12- and 24-h treatments, respectively. 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. Ethaselen (2.5-50 μM; 1-24 hours) causes intracellular Trx oxidation in A549 cells. Ethaselen (5-10 μM; 12, 24 hours) causes a clear concentration-dependent increase in ROS levels in A549 cells. The inhibition constants for Ethaselen binding to free enzyme (K i ) and the enzyme-substrate complex (K is ) 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell 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\t(BBSKE; 36-108 mg/kg/day; PO; for 10 days) shows increased inhibition of tumor growth in a dose-independent manner. 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 cellDosage: 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). IC50& Target:TrxR |
| Isomeric SMILES | C1=CC=C2C(=C1)C(=O)N([Se]2)CCN3C(=O)C4=CC=CC=C4[Se]3 |
|---|---|
| 关联CAS | 217798-39-5 |
| PubChem CID | 10387485 |
| MeSH Entry Terms | (1,2-bis(1,2-benzisoselenazolone-3(2H)-ketone))ethane;BBSKE cpd;ethaselen |
| 分子量 | 422.20 |
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