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Ethaselen

CAS No. : 217798-39-5

MCE 站：Ethaselen

产品活性：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。

研究领域：Others

作用靶点：Others

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 IC₅₀ 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.

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

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