Galiellalactone-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEGaliellalactoneCat.No.:HY-125170CASNo.:133613-71-5分?式:C??H??O?分?量:194.23作?靶點:STAT作?通路:JAK/STATSignaling;StemCell/Wnt儲存?式:PleasestoretheproductundertherecommendedconditionsintheCOA.BIOLOGICALACTIVITY?物活性Galiellalactone?種?的?毒且?致突變性的真代謝產(chǎn)物，?種選擇性的STAT3信號抑制劑，IC50值為250-500nM。Galiellalactone可?于研究去勢抵抗性前列腺癌。IC50&TargetSTAT3250-500nM(IC50)體外研究Galiellalactone(2.5-25μM;24-72hour)inducesapoptosisofprostatecancer(PCa)celllinesexpressingp-Stat3[1].Galiellalactone(2.5-25μM;24-72hour)decreasesviabilityofDU145cells[1].Galiellalactone(10μM)inhibitsSTAT3signalingactivityasassessedbyluciferasereportergeneassayinIL-6-stimulatedLNCaPcells[2].Galiellalactone(10-100μM;1hour)bindsdirectlytoSTAT3inDU145cells[2].Galiellalactone(5-50μM;1hour)interfereswithSTAT3DNAbindingwithoutinhibitingphosphorylationinDU145cells[2].ApoptosisAnalysis[1]CellLine:DU145,PC-3,andLNCaPcellsConcentration:0,2.5,5,10,25μMIncubationTime:24,48,72hoursResult:InducedanapoptoticresponseinPC-3andDU145cells.1/3MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemECellViabilityAssay[1]CellLine:DU145cellsConcentration:0,2.5,5,10,17.5,25μMIncubationTime:24,48,72hoursResult:DecreasedDU145cellsviabilityinadose-andtime-dependentmanner.WesternBlotAnalysis[1]CellLine:DU145cellsConcentration:0,10,25μMIncubationTime:48hoursResult:Inducedexpressionoftheapoptoticmarkercleavedcaspase-3andincreasedexpressionofcleavedPARP.WesternBlotAnalysis[2]CellLine:DU145cellsConcentration:0,10,25,50,100μMIncubationTime:1hourResult:Preventedthebindingofthebiotinylatedanalogueofgaliellalactone(GL-biot)toSTAT3inadose-dependentmannerdemonstratingcompetitivebinding.WesternBlotAnalysis[2]CellLine:DU145cellsConcentration:0,5,10,25,50μMIncubationTime:1hourResult:InhibitedSTAT3bindingtoDNAinadose-dependentmanner.DidnotaffectphosphorylationofSTAT3Tyr-705andSer-727ortheexpressionoftotalSTAT3.體內研究Galiellalactone(1,3?mg/kg;dailyi.p.for3weeks)inhibitsPCatumorgrowthinvivo[1].AnimalModel:MalenudeNMR1miceareinjectedPCacell[1]Dosage:0,1,3?mg/kg2/3MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemEAdministration:Dailyi.p.injectionsfor3weeksResult:ReducedthetumorgrowthrateinDU145xenograftsby41-42%andwaswelltolerated.REFERENCES[1].HellstenR,et,al.Galiellalactoneisanoveltherapeuticcandidateagainsthormone-refractoryprostatecancerexpressingactivatedStat3.Prostate.2008Feb15;68(3):269-80.[2].DoncowDN,et,al.GaliellalactoneisadirectinhibitorofthetranscriptionfactorSTAT3inprostatecancercells.JBiolChem.2014Jun6;289(23):15969-78.[3].WeidlerM,et,al.Inhibitionofinterleukin-6signalingbygaliellalactone.FEBSLett.2000Oct27;484(1):1-6.McePdfHeightCaution:Producthasnotbeenfullyvalidated