Acacetin-5-7-Dihydroxy-4-methoxyflavone-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAcacetinCat.No.:HY-N0451CASNo.:480-44-4Synonyms:5,7-Dihydroxy-4'-methoxyflavone分⼦式:C₁₆H₁₂O₅分⼦量:284.26作⽤靶点:Apoptosis;Autophagy作⽤通路:Apoptosis;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(439.74mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.5179mL17.5895mL35.1791mL5mM0.7036mL3.5179mL7.0358mL10mM0.3518mL1.7590mL3.5179mL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>>90%cornoil1/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(7.32mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Acacetin(5,7-Dihydroxy-4'-methoxyflavone)⼀种⼝服有效的类酮，来⾃Dendranthemamorifolium。Acacetin停在PI3Kγ的ATP结合⼝袋中。Acacetin导致癌细胞周期停滞，并诱导细胞凋亡和⾃噬。Acacetin具有有效的抗癌和抗炎活性，有⽤于疼痛相关疾病研究的潜⼒。体外研究Acacetin(5,7-Dihydroxy-4'-methoxyflavone;10-200μM;24hours)decreasescellviabilitiesinadose-dependentmanner.AcacetinhaslittleeffectonhumannormalglialcelllineHEBandnon-tumorigenicepithelialcelllineMCF-10A[1].Acacetin(50-150μM;24hours)causesG2/Mcellcyclearrestandinducesapoptosisandautophagy[1].Acacetin(50-150μM;24hours)leadstodecreasesinlevelsofPI3Kγ-p110,p-AKT,p-mTOR,p-p70S6K,andp-ULKinadose-dependentmanner[1].CellViabilityAssay[1]CellLine:BreastcancerMCF-7cells,hepatocellularcarcinomaSMMC-7721cells,lungadenocarcinomaA549cells,esophagealcarcinomaEca109cellsConcentration:10,20,40,60,80,100,150,200μMIncubationTime:24hoursResult:Decreasedcancercellviabilitiesinadose-dependentmanner.HadIC50valuesof82.75ꢀμM,103.9μM,157.4μM,54.7μMinMDA-MB-231,MCF-7,A549,Eca109cells,respectively.CellCycleAnalysis[1]CellLine:MDA-MB-231cellsConcentration:50,100,150μMIncubationTime:24hoursResult:ResultedinincreaseinpercentageofcellsatG2/MphaseanddecreaseinpercentageofcellsatG1andSphaseinadose-dependentmanner.ApoptosisAnalysis[1]CellLine:MDA-MB-231cellsConcentration:50,100,150μMIncubationTime:24hours2/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:Inducedapoptosis.CellAutophagyAssay[1]CellLine:MDA-MB-231cellsConcentration:50,100,150μMIncubationTime:24hoursResult:Inducedautophagy.ResultedinmarkedincreasesinEGFP-LC3punctaformationandadose-dependentaccumulationofLC3-II.WesternBlotAnalysis[1]CellLine:MDA-MB-231cellsConcentration:50,100,150μMIncubationTime:24hoursResult:ResultedindecreaseinlevelsofBcl-2andBcl-xLandincreaseinlevelsofp53.LedtodecreasesinlevelsofPI3Kγ-p110,p-AKT,p-mTOR,p-p70S6K,andp-ULKinadose-dependentmanner.HadlittleornoeffectonexpressionofPI3Kα,PI3Kβ,PI3Kδ,p-ERK,p-p38,andp-JNK.体内研究Acacetin(5,7-Dihydroxy-4'-methoxyflavone;5,20mg/kg/day;orally;for3days)significantlysuppressesmicroglialactivationinanLPS-inducedneuroinflammationmousemodel[2].Acacetin(25mg/kg/day;orally;for3days)reducesneuronalcelldeathinananimalmodelofischemia[2].Acacetin(1.8-56.2mg/kg/day;ip;singledose)decreasesvisceralandinflammatorynociceptionandpreventedtheformalin-inducedoedema[3].AnimalModel:MaleC57BL/6mice,7weeksofage[2]Dosage:5,20mg/kgAdministration:Orally;onceadayfor3daysResult:SignificantlysuppressedmicroglialactivationinanLPS-induced(ip;5mg/kg)neuroinflammationmousemodel.户使⽤本产品发表的科研⽂献•ActaPharmSinB.2021Jan;11(1):143-155.3/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•PharmacolRes.2020May;155:104751.•EMBORep.2022Apr11;e53932.•FutureMicrobiol.2020May;15:485-496.•BiolPharmBull.2022;45(8):1116-1123.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].Hong-WeiZhang,etal.FlavonoidsinhibitcellproliferationandinduceapoptosisandautophagythroughdownregulationofPI3KγmediatedPI3K/AKT/mTOR/p70S6K/ULKsignalingpathwayinhumanbreastcancercells.SciRep.2018Jul26;8(1):11255.[2].SangKeunHa,etal.AcacetinattenuatesneuroinflammationviaregulationtheresponsetoLPSstimuliinvitroandinvivo.NeurochemRes.2012Jul;37(7):1560-7.[3].AICarballo-Villalobos,etal.Evidenceofmechanismofactionofanti-inflammatory/antinociceptiveactivitiesofacacetin.EurJPai