Hinokitiol-β-Thujaplicin-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEHinokitiolCat. No.: HY-B2230CAS No.: 499-44-5Synonyms: -Thujaplicin分式: CHO分量: 164.2作靶點(diǎn): Keap1-Nrf2; DNA Methyltransferase作通路: NF-B; Epigenetics儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO

2、: 100 mg/mL (609.01 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (15.23 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (15.23 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubilit

3、y: 2.5 mg/mL (15.23 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Hinokitiol從本扁柏中分離到的揮發(fā)油成分，能夠降低 Nrf2 的表達(dá)，減少 DNMT1 和 UHRF1 的 mRNA 和蛋的表達(dá)，具有抗感染、抗氧化及抗腫瘤等活性。IC50 & Target DNMT1 Nrf2體外研究 In U87MG and T98G glioma cell lines, hinokitiol demonstrates a dose-dependent decrease in viability, withIC50 values of 316

4、.5 35.5 and 152.5 25.3 M, respectively. Hinokitiol represses ALDH activity and self-renewal ability in glioma stem cells, and inhibits in vitro oncogenicity. Hinokitiol also reduces Nrf2 expressionin glioma stem cells in a dose-dependent manner 1. Hinokitiol (0-100 M) inhibits colon cancer cell grow

5、thin a dose- and time-dependent manner. Hinokitiol (5, 10 M) decreases DNMT1 and UHRF1 mRNA andprotein expression, and increases TET1 expression via enhancement of 5hmC level in HCT-116 cells.Furthermore, hinokitiol reduces methylation status and restores mRNA expression of MGMT, CHST10, andBTG4 gen

6、es 2.PROTOCOLCell Assay 1 U87MG and T98G glioma cells are cultured in Dulbeccos modified Eagles medium with Hams F12 medium(DMEM/F-12) containing 10% fetal bovine serum. Cell viability is determined using MTT to evaluate thecytotoxicity of hinokitiol. Cells are seeded in 24-well plates (1105 cells/w

7、ell) in the presence of variousconcentration of hinokitiol or vehicle at 37C for 24 h followed by incubation with MTT reagent. The blueformazan crystals of viable cells are dissolved in DMSO and then evaluated spectrophotometrically at 570nm. DMSO-treated group is set as 100%, and data are presented

8、 as percentage of DMSO control. IC50values are calculated by the GraFit software.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Ouyang WC, et al. Hinokitiol suppresses cancer stemness and oncogenicity in glioma stem cells by Nrf2 regulation. Cancer ChemotherPharmacol. 2017 Aug;80(2):411-419.2. Seo JS, et al. Hinokitiol induces DNA demethylation via DNMT1 and UHRF1 inhibition in colon cancer cells. BMC Cell Biol. 2017 Feb27;18(1):14.McePdfHeightCaution: Product has not been fully validated for medical ap