8-Hydroxy-efavirenz

8-Hydroxyefavirenz (8-OH-EFV) is a primary metabolite of Efavirenz (HY-10572). 8-Hydroxyefavirenz induces apoptosis via a JNK- and BimEL-dependent mechanism in primary human hepatocytes. 8-Hydroxyefavirenz can be used in research of cancer[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> MAPK/ERK Pathway >> JNK

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.

[1]. Bumpus NN. Efavirenz and 8-hydroxyefavirenz induce cell death via a JNK- and BimEL-dependent mechanism in primary human hepatocytes. Toxicol Appl Pharmacol. 2011 Dec 1;257(2):227-34.