Isosilybin-Isosilybinin-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEIsosilybinCat. No.: HY-N0779CAS No.: 72581-71-6Synonyms: Isosilybinin分式: CHO分量: 482.44作靶点: Cytochrome P450作通路: Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 28 mg

2、/mL (58.04 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.0728 mL 10.3640 mL 20.7280 mL5 mM 0.4146 mL 2.0728 mL 4.1456 mL10 mM 0.2073 mL 1.0364 mL 2.0728 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Isosilybin (Isosilybinin)来乳蓟

3、的类黄酮；抑制CYP3A4诱导的IC50值为74 M。IC50 & Target IC50: 74 M (CYP3A4) 1体外研究The reporter gene assay shows that milk thistles components silybin and isosilybin are responsible for the1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEinhibition of PXR-mediated CYP3A4 induction by milk thistle. Compared with sily

4、bin, its isomer isosilybin is astronger inhibitor of PXR-mediated CYP3A4 induction. A solution of 89, 133, and 200 M isosilybinsignificantly inhibits CYP3A4 induction by 64, 82, and 88%, respectively. Isosilybin inhibits CYP3A4 inductionwith an IC50 of 74 M 1. Isosilybin B and isosilybin A, two dias

5、tereoisomers isolated from silymarin, haveanti-prostate cancer (PCA) activity that is mediated via cell cycle arrest and apoptosis induction. Isosilybin Band isosilybin A treatment results in growth inhibition and cell death together with a strong G(1) arrest andapoptosis in human prostate cancer LN

6、CaP and 22Rv1 cells 2. Isosilybin B causes increasedphosphorylation of Akt (Ser-473 and Thr-308) and Mdm2 (Ser-166), which is linked with androgen receptordegradation as pretreatment with PI3K inhibitor (LY294002)-restored androgen receptor level. Isosilybin Btreatment enhances the formation of comp

7、lex between Akt, Mdm2 and AR, which promotes phosphorylation-dependent AR ubiquitination and its degradation by proteasome 3. Isosilybin A is able to significantlyactivate PPAR at a concentration of 30 M (2.080.48 fold, p 4.PROTOCOLCell Assay 2 LNCaP cells and 22Rv1 cells are plated and treated at 4

8、050% confluency with different doses of isosilybinB and isosilybin A (1090 M in medium) dissolved originally in Dimethyl sulfoxide (DMSO) for the desiredtime periods (2448 h) in serum condition. An equal amount of DMSO (vehicle) is present in each treatment,including control; DMSO concentration did

9、not exceed 0.1% (v/v) in any treatment. At the end of desiredtreatments, total cell number is determined by counting each sample in duplicate using a hemocytometerunder an inverted microscope. Cell viability is determined using trypan blue exclusion method 2.MCE has not independently confirmed the a

10、ccuracy of these methods. They are for reference only.REFERENCES1. Mooiman KD, et al. Milk thistles active components silybin and isosilybin: novel inhibitors of PXR-mediated CYP3A4 induction. DrugMetab Dispos. 2013 Aug;41(8):1494-504.2. Deep G, et al. Isosilybin B and isosilybin A inhibit growth, i

11、nduce G1 arrest and cause apoptosis in human prostate cancer LNCaP and22Rv1 cells. Carcinogenesis. 2007 Jul;28(7):1533-42.3. Deep G, et al. Isosilybin B causes androgen receptor degradation in human prostate carcinoma cells via PI3K-Akt-Mdm2-mediatedpathway. Oncogene. 2008 Jun 26;27(28):3986-98.4. Pferschy-Wenzig EM, et al. Identification of isosilybin a from milk thistle seeds as an agonist of peroxisome proliferator-activatedreceptor gamma. J Nat Prod. 2014 Apr 25;77(4):842-7.McePdfHeightCaution: Product