Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAcacetinCat.No.:HY-N0451CASNo.:480-44-4Synonyms:5,7-Dihydroxy-4'-methoxyflavone分?式:C??H??O?分?量:284.26作?靶點:Apoptosis;Autophagy作?通路:Apoptosis;Autophagy儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數據體外實驗DMSO:125mg/mL(439.74mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.5179mL17.5895mL35.1791mL5mM0.7036mL3.5179mL7.0358mL10mM0.3518mL1.7590mL3.5179mL請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現?現配，當天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現沉淀、析出現象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>90%cornoil1/4MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(7.32mM);ClearsolutionBIOLOGICALACTIVITY?物活性Acacetin(5,7-Dihydroxy-4'-methoxyflavone)?種?服有效的類酮，來?Dendranthemamorifolium。Acacetin停在PI3Kγ的ATP結合?袋中。Acacetin導致癌細胞周期停滯，并誘導細胞凋亡和?噬。Acacetin具有有效的抗癌和抗炎活性，有?于疼痛相關疾病研究的潛?。體外研究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.HadIC50valuesof82.75?μM,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?邊的抑制劑?師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.體內研究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.戶使?本產品發表的科研?獻?ActaPharmSinB.2021Jan;11(1):143-155.3/4MasterofBioactiveMolecules—您?邊的抑制劑?師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