Galangin-Norizalpinin-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGalanginCat.No.:HY-N0382CASNo.:548-83-4Synonyms:Norizalpinin;3,5,7-Trihydroxyflavone分⼦式:C₁₅H₁₀O₅分⼦量:270.24作⽤靶点:CytochromeP450;Autophagy;Autophagy作⽤通路:MetabolicEnzyme/Protease;Autophagy储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:125mg/mL(462.55mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.7004mL18.5021mL37.0041mL5mM0.7401mL3.7004mL7.4008mL10mM0.3700mL1.8502mL3.7004mL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；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(7.70mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Galangin(Norizalpinin)arylhydrocarbon受体的调节剂，同时抑制CYP1A1的活性。IC50&TargetCYP1体外研究Galangin(Norizalpinin)inhibitsthecatabolicbreakdownofDMBA,asmeasuredbythin-layerchromatography,inadose-dependentmanner.GalanginalsoinhibitstheformationofDMBA-DNAadducts,andpreventsDMBA-inducedinhibitionofcellgrowth.Galangincausesapotent,dose-dependentinhibitionofCYP1A1activity,asmeasuredbyethoxyresorufin-O-deethylaseactivity,inintactcellsandinmicrosomesisolatedfromDMBA-treatedcells.Analysisoftheinhibitionkineticsbydouble-reciprocalplotdemonstratesthatgalangininhibitsCYP1A1activityinanoncompetitivemanner.GalangincausesanincreaseinthelevelofCYP1A1mRNA,indicatingthatitmaybeanagonistofthearylhydrocarbonreceptor,butitinhibitstheinductionofCYP1A1mRNAbyDMBAorby2,3,5,7-tetrachlorodibenzo-p-dioxin(TCDD).GalanginalsoinhibitstheDMBA-orTCDD-inducedtranscriptionofareportervectorcontainingtheCYP1A1promoter[1].Galangintreatmentinhibitscellproliferationandinducedautophagy(130μM)andapoptosis(370μM).Inparticular,galangintreatmentinHepG2cellscauses(1)anaccumulationofautophagosomes,(2)elevatedlevelsofmicrotubule-associatedproteinlightchain3,and(3)anincreasedpercentageofcellswithvacuoles.p53expressionisalsoincreased.Thegalangin-inducedautophagyisattenuatedbytheinhibitionofp53inHepG2cells,andoverexpressionofp53inHep3Bcellsrestoredthegalangin-inducedhigherpercentageofcellswithvacuolestonormallevel[2].PROTOCOLCellAssay[2]Cells(5.0×103)areseededandtreatedwithdifferentconcentrationsofgalanginfordifferentperiodsoftimein96-wellplates.Thenumberofviablecellsineachwellisdeterminedbyadding10µLof5mg/mLMTTsolution.Followingthe4hourincubationat37°C,thecellsaredissolvedina100µLsolutioncontaining20%SDSand50%dimethyformamide.Theopticaldensitiesarequantifiedatatestwavelengthof570nmwithareferencewavelengthof630nmusingaVarioskanFlashReaderspectrophotometer.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•ActaPharmSinB.2021Jan;11(1):143-155.•PharmacolRes.2020May;155:104751.•EurJPharmacol.2021Jun3;174232.•DrugDesDevTher.2020Aug19;14:3393-3405.•AmJTranslRes.2021Aug15;13(8):8742-8753.Seemorecustomervalidationsonwww.MedChemE2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEREFERENCES[1].CiolinoHP,etal.TheflavonoidgalanginisaninhibitorofCYP1A1activityandanagonist/antagonistofthearylhydrocarbonreceptor.BrJCancer.1999Mar;79(9-10):1340-6.[2].WenM,etal.Galangininducesautophagythroughupregulationofp53inHepG2cells.Pharmacology.2012;89(5-6):247-55.McePdfHeightC