8-Hydroxyefavirenz 是 Efavirenz (HY-10572) 的主要代谢物，8-Hydroxyefavirenz 通过 JNK 和 BimEL 依赖机制诱导原代人肝细胞凋亡 (apoptosis)。8-Hydroxyefavirenz 可用于癌症研究。
| 生物活性 | 8-Hydroxyefavirenz (8-OH-EFV) is a primary metabolite ofEfavirenz(HY-10572). 8-Hydroxyefavirenz inducesapoptosisvia a JNK- and BimEL-dependent mechanism in primary human hepatocytes. 8-Hydroxyefavirenz can be used in research ofcancer[1]. |
体外研究
(In Vitro) | 8-Hydroxyefavirenz (8-OH-EFV; 1-10 μM; 3-24 h; 原代人肝细胞) 以时间和浓度依赖的方式增加细胞死亡，并从 6 小时开始诱导 caspase-3 活性[1]。
8-Hydroxyefavirenz (1-10 μM; 6-24 h) 刺激原代人肝细胞中线粒体 ROS 的产生[1]。
8-Hydroxyefavirenz (10 μM; 3-24 h) 激活 JNK 并使磷酸化的 JNK 占总 JNK 的比例增加 4.2 倍。8-Hydroxyefavirenz 增加 BimEL mRNA 和蛋白表达[1]。
Cell Viability Assay[1] | Cell Line: | Primary human hepatocytes | | Concentration: | 1 and 10 μM | | Incubation Time: | 3, 6, 12 and 24 hours | | Result: | Increased cell death in a time- and concentration-dependent manner and increased cell death by 3.4-fold at 6 h. |
Western Blot Analysis[1] | Cell Line: | Primary human hepatocytes | | Concentration: | 1 and 10 μM | | Incubation Time: | 3, 6, 12 and 24 hours | | Result: | Increased the expression of cleaved caspase-3 in a time- and concentration-dependent manner. |
Western Blot Analysis[1] | Cell Line: | Primary human hepatocytes | | Concentration: | 1 and 10 μM | | Incubation Time: | 3, 6, 12 and 24 hours | | Result: | Increased the phosphorylation of JNK and increased the mRNA and protein expression of BimEL. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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