HP590-DataSheet-生命科學(xué)試劑-MCE

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEHP590Cat.No.:HY-151480分?式:C??H??F?N?O?分?量:590.52作?靶點(diǎn):STAT;Apoptosis作?通路:JAK/STATSignaling;StemCell/Wnt;Apoptosis儲(chǔ)存?式:4°C,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoistureandlight)BIOLOGICALACTIVITY?物活性HP590?種具有?服活性的、新型和強(qiáng)效的STAT3抑制劑(STAT3熒光素酶活性:IC50=27.8nM;ATP抑制:IC50=24.7nM)。HP590對胃癌細(xì)胞顯?出抗增殖活性并可誘導(dǎo)細(xì)胞凋亡。IC50&TargetIC50:27.8nM(STAT3luciferaseactivity)[1]體外研究HP590(0-40μM;72h)showsanti-proliferativeactivitiestoMKN45,AGS,andMGC803cells[1].HP590(0-40nM;0-24h)inhibitsSTAT3Tyr705andSer727phosphorylationinGCcells,blockstheexpressionofSTAT3downstreamgenes(c-MycandcyclinD1)inGCcells,reducesIL-6-mediatedSTAT3nucleartranslocationinMKN45cells[1].HP590(5-20nM;48h)inducesgastriccancercellapoptosis[1].CellProliferationAssay[1]CellLine:MKN45,AGS,andMGC803cellsConcentration:0-40μMIncubationTime:72hoursResult:InhibitedMKN45,AGS,andMGC803cellswithIC50sof9.3,13.5,and8.7nM,respectively.ApoptosisAnalysis[1]CellLine:MKN45andAGScells1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEConcentration:5,10,and20nMIncubationTime:48hoursResult:InducedapoptosisinMKN45andAGScellsinadose-dependentmanner.WesternBlotAnalysis[1]CellLine:GastricCancerCellsConcentration:0-40nMIncubationTime:0-24hResult:InhibitedSTAT3p-Tyr705andp-Ser727inGCcellscompletelyat40nM.BlockedtheexpressionofSTAT3downstreamgenes,includingc-MycandcyclinD1,inaconcentration-dependentandtime-dependentmanner.ShowedtheSTAT3p-Tyr705stimulatedbyIL-6inGCcelllines,butentirelysuppressedbyHP590at40nM.RT-PCR[1]CellLine:MKN45andAGScellsConcentration:10,20,and40nMIncubationTime:48hoursResult:SuppressedtheexpressionofSTAT3downstreamgenes(c-MycandcyclinD1)atthemRNAlevel.體內(nèi)研究HP590(oraladministration;25and50mg/kg;oncedaily;5w)inhibitsGCgrowtheffectivelybyinhibitingtheSTAT3activationandshowsbettertoleranceinGCxenograftmodel[1].AnimalModel:BALB/c-nudemiceinjectedwithGCcells[1]Dosage:25and50mg/kgAdministration:Oraladministration;25and50mg/kg;oncedaily;5weeksResult:InhibitedMKN45tumorgrowthinaconcentration-dependentmanner.InhibitedSTAT3phosphorylationatTyr705andSer727andreducedtheexpressionofthedownstreamgenes.InhibitedtheexpressionofKi67(aproliferationmarker).ShowednoweightlossduringHP590treatment,andnoapparentdamageinthemajororgansofmice.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEREFERENCES[1].HeP,etal.DiscoveryofaNovelPotentSTAT3InhibitorHP590withDualp-Tyr705/Ser727InhibitoryActivityforGastricCancerTreatment.JMedChem.2022Sep14.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformed