Galangin-Norizalpinin-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGalanginCat. No.: HY-N0382CAS No.: 548-83-4Synonyms: Norizalpinin; 3,5,7-Trihydroxyflavone分式: CHO分量: 270.24作靶點(diǎn): Cytochrome P450; Autophagy; Autophagy作通路: Metabolic Enzyme/Protease; Autophagy儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn s

2、olvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 36 mg/mL (133.21 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 3.7004 mL 18.5021 mL 37.0041 mL5 mM 0.7401 mL 3.7004 mL 7.4008 mL10 mM 0.3700 mL 1.8502 mL 3.7004 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式

3、和期限。BIOLOGICAL ACTIVITY物活性 Galangin是arylhydrocarbon 受體的調(diào)節(jié)劑，同時(shí)抑制 CYP1A1 的活性。體外研究Galangin inhibits the catabolic breakdown of DMBA, as measured by thin-layer chromatography, in a dose-dependent manner. Galangin also inhibits the formation of DMBA-DNA adducts, and prevents DMBA-induced inhibition of ce

4、ll growth. Galangin causes a potent, dose-dependent inhibition of CYP1A1 activity, as1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEmeasured by ethoxyresorufin-O-deethylase activity, in intact cells and in microsomes isolated from DMBA-treated cells. Analysis of the inhibition kinetics by double-r

5、eciprocal plot demonstrates that galangin inhibitsCYP1A1 activity in a noncompetitive manner. Galangin causes an increase in the level of CYP1A1 mRNA,indicating that it may be an agonist of the aryl hydrocarbon receptor, but it inhibits the inductionof CYP1A1 mRNA by DMBA or by 2,3,5,7-tetrachlorodi

6、benzo-p-dioxin (TCDD). Galangin also inhibits theDMBA- or TCDD-induced transcription of a reporter vector containing the CYP1A1 promoter 1. Galangintreatment inhibits cell proliferation and induced autophagy (130 M) and apoptosis (370 M). In particular,galangin treatment in HepG2 cells causes (1) an

7、 accumulation of autophagosomes, (2) elevated levels ofmicrotubule-associated protein light chain 3, and (3) an increased percentage of cells with vacuoles. p53expression is also increased. The galangin-induced autophagy is attenuated by the inhibition of p53 inHepG2 cells, and overexpression of p53

8、 in Hep3B cells restored the galangin-induced higher percentage ofcells with vacuoles to normal level 2.PROTOCOLCell Assay 2 Cells (5.0103) are seeded and treated with different concentrations of galangin for different periods of timein 96-well plates. The number of viable cells in each well is dete

9、rmined by adding 10 L of 5 mg/mL MTTsolution. Following the 4 hour incubation at 37C, the cells are dissolved in a 100 L solution containing 20%SDS and 50% dimethy formamide. The optical densities are quantified at a test wavelength of 570 nm with areference wavelength of 630 nm using a Varioskan Fl

10、ash Reader spectrophotometer.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Ciolino HP, et al. The flavonoid galangin is an inhibitor of CYP1A1 activity and an agonist/antagonist of the aryl hydrocarbon receptor. BrJ Cancer. 1999 Mar;79(9-10):1340-6.2. Wen M, et al. Galangin induces autophagy through upregulation of p53 in HepG2 cells. Pharmacology. 2012;89(5-6):247-55.McePdfHeightCaution: Product has not been ful