MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务。
CAS No. : 217798-39-5
MCE 国际站: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活性分子,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:Metabolic Enzyme/Protease
作用靶点: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 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 (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.
In Vivo: Ethaselen (BBSKE; 36-108 mg/kg/day; PO; for 10 days) shows increased inhibition of tumor growth in a dose-independent manner.
相关产品:Clinical Compound Library Plus | Bioactive Compound Library Plus | Metabolism/Protease Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Orally Active Compound Library | Anti-Lung Cancer Compound Library | 8α-Tigloyloxyhirsutinolide 13-O-acetate | TRFS-green | TrxR-IN-3 | TrxR-IN-4 | DVD-445 | CPUL1 | PMX464 | TrxR-IN-2 | TP-TRFS | ROS-generating agent 1
热门产品线:重组蛋白 | 化合物库 | 天然产物 | 荧光染料 | PROTAC | 同位素标记物 | 寡核苷酸 | 抗体 | 点击化学
Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides | Antibodies | Click Chemistry
货号: HY-116749
品牌介绍:
• MCE (MedChemExpress) 拥有200 多种全球独家化合物库,我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物;
• 50,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领;
• 产品种类涵盖各种重组蛋白,多肽,常用试剂盒 ,更有 PROTAC、ADC 等特色产品,广泛应用于新药研发、生命科学等科研项目;
• 提供虚拟筛选,离子通道筛选,代谢组学分析检测分析,药物筛选等专业技术服务;
• 设有专业的实验中心和严格的质控、验证体系;
• 提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告,确保产品的高纯度、高品质;
• 产品的生物活性多经各国客户实验验证;
• Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果;
• 专业团队跟踪最新的制药及生命科学研究进展,为您提供全球最新的活性化合物;
• 与世界各大制药公司及知名科研机构建立了长期的合作。