Isosilybin 产品活性：Isosilybin (Isosilybinin)是来自水飞蓟的类黄酮；抑制CYP3A4诱导的IC50值为74 μM。 产品来源： https://www.medchemexpress.cn/Isosilybin.html 研究领域：Metabolic Enzyme/Protease 作用靶点：Cytochrome P450 来源：植物 | 豆科 | Glycine soya | 植物 | 豆科 | 瓜儿豆 | 植物 | 菊科 结构分类：黄酮类 | 二氢黄酮醇 | 酚类 | 多酚类 In Vitro: The reporter gene assay shows that milk thistle’s components silybin and isosilybin are responsible for the inhibition of PXR-mediated CYP3A4 induction by milk thistle. Compared with silybin, its isomer isosilybin is a stronger inhibitor of PXR-mediated CYP3A4 induction. A solution of 89, 133, and 200 μM isosilybin significantly inhibits CYP3A4 induction by 64, 82, and 88%, respectively. Isosilybin inhibits CYP3A4 induction with an IC50 of 74 μM. Isosilybin B and isosilybin A, two diastereoisomers isolated from silymarin, have anti-prostate cancer (PCA) activity that is mediated via cell cycle arrest and apoptosis induction. Isosilybin B and isosilybin A treatment results in growth inhibition and cell death together with a strong G(1) arrest and apoptosis in human prostate cancer LNCaP and 22Rv1 cells. Isosilybin B causes increased phosphorylation of Akt (Ser-473 and Thr-308) and Mdm2 (Ser-166), which is linked with androgen receptor degradation as pretreatment with PI3K inhibitor (LY294002)-restored androgen receptor level. Isosilybin B treatment enhances the formation of complex between Akt, Mdm2 and AR, which promotes phosphorylation-dependent AR ubiquitination and its degradation by proteasome. Isosilybin A is able to significantly activate PPARγ at a concentration of 30 μM (2.08±0.48 fold, p<0.01). Isosilybin A causes transactivation of a PPARγ-dependent luciferase reporter in a concentration-dependent manner. In silico docking studies suggests a binding mode for 3 distinct from that of the inactive silymarin constituents, with one additional hydrogen bond to Ser342 in the entrance region of the ligand-binding domain of the receptor. 相关产品：Natural Product Library Plus | Bioactive Compound Library Plus | Metabolism/Protease Compound Library | Natural Product Library | Anti-Cancer Compound Library | Anti-Aging Compound Library | Antioxidant Compound Library | Oxygen Sensing Compound Library | Medicine Food Homology Compound Library | Phenols Library | Traditional Chinese Medicine Active Compound Library | Flavonoids Library | Mitochondria-Targeted Compound Library | Food-Sourced Compound Library | Anti-Cancer Natural Product Library | Plant-Sourced Natural Product Library | Human Metabolite Library | Metabolic Enzyme Compound Library | Radioprotector Library | Bioactive Compound Library Max | Verapamil | Apigenin | Fenofibrate | Chlorpromazine hydrochloride | Ketoconazole | Abiraterone | Letrozole | 1-Aminobenzotriazole | Itraconazole | Cepharanthine | Quinidine (15% dihydroquinidine) | Clarithromycin | Atovaquone | Diosmetin | Gemfibrozil 1-O-β-glucuronide | Naringin | Fomepizole | Talarozole | Hypericin | Salvianolic acid C | Methoxsalen | HET0016 | Memantine hydrochloride | Anastrozole | (S)-Mephenytoin | Sulfaphenazole | Cobicistat 品牌介绍: MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供最新最全的高品质小分子活性化合物；10,000 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域；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。