HS-1793-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEHS-1793Cat.No.:HY-129156CASNo.:927885-00-5分?式:C??H??O?分?量:252.26作?靶點(diǎn):Apoptosis作?通路:Apoptosis儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性HS-1793?種Resveratrol類(lèi)似物，在多種癌細(xì)胞中具有抗腫瘤活性[1]。HS-1793誘導(dǎo)細(xì)胞凋亡(apoptosis)。體外研究HS-1793(0-100μM;24h)suppressesproliferationofMCF-7,MDA-MB-231andHCT116cells[1][2].HS-1793(0-50μM;4h)inhibitshypoxia-inducedHIF-1αproteininMCF-7andMDA-MB-231cellsunrelatedtocelldeath,downregulateshypoxia-inducedVEGFexpression,andsuppresseshypoxia-inducedmRNAexpressionofVEGFatthetranscriptionallevel[1].HS-1793(0-100μM;24h)inducesapoptosis,promotesG2/Mcellcyclearrest,andinhibitsAktandERKphosphorylationinHCT116cells[2].CellProliferationAssay[1]CellLine:MCF-7,MDA-MB-231andMCF-10AConcentration:0-100μMIncubationTime:24hResult:ShowedantiproliferationactivitywithIC50valuesof26.3±3.2,48.2±4.2and>100μMagainstMCF-7,MDA-MB-231andMCF-10A,respectively.WesternBlotAnalysis[1]CellLine:MCF-7,MDA-MB-2311/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEConcentration:12.5,25and50μMIncubationTime:4hResult:DownregulatedHIF-1αexpressioninaconcentration-dependentmannerinbothcelllines.RT-PCR[1]CellLine:MCF-7,MDA-MB-231Concentration:12.5,25and50μMIncubationTime:4hResult:DownregulatedtheexpressionofVEGFmRNA,withthemoremarkedresultsobservedinMDA-MB-231cells.CellProliferationAssay[2]CellLine:HCT116Concentration:12.5,25,50and100μMIncubationTime:1,2and4daysResult:Significantlyreducedthecellviabilityconcentration-andtime-dependently.SignificantlysuppressedproliferationofcoloncancercelllineHCT116.ApoptosisAnalysis[2]CellLine:HCT116Concentration:12.5,25,50and100μMIncubationTime:24hResult:Inducedcellapoptosisinadose-dependentmanner.Causedchromatincondensationandfragmentation.WesternBlotAnalysis[2]CellLine:HCT116Concentration:12.5,25,50and100μMIncubationTime:24hResult:Effectivelyinducedthereductionofpro-caspase-8andpro-caspase-3at100μM.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEActivatedcaspase-8andcaspase-3.CausedthePARPcleavage.SlightlydownregulatedthelevelofantiapoptoticproteinBcl-2at100μM.Promotedanincreaseinthereleaseofcytochromecfromthemitochondriaintothecytosol.DecreasedtheexpressionofG2/McellcycleregulatoryproteincyclinB1,Cdc2andCdc25C.DecreasedthelevelofCDK4andCDK6.DecreasedAktphosphorylationandreducedtotalAktathigh-concentration.DecreasedthephosphorylationofERK1/2withoutaffectingtheproteinlevel.CellCycleAnalysis[2]CellLine:HCT116Concentration:12.5,25and50μMIncubationTime:24hResult:InducedtheaccumulationofcellsintheG2/Mphaseinaconcentration-dependentmanner.體內(nèi)研究HS-1793(5and10mg/kg;i.p.;twiceaweek,4weeks)significantlyinhibitsMDA-MB-231xenografttumorgrowthandinadose-dependentmannerandrelativelyhampersangiogenesiswithnon-toxicity[1].AnimalModel:Five-week-oldfemaleBALB/cnudemiceinjectedwithMDA-MB-231cells[1]Dosage:5mg/kgand10mg/kg(dissolvedinPBScontaining0.1%v/vdimethylsulfoxide(DMSO))Administration:Intraperitonealinjection,twiceaweek,4weeksResult:SignificantlyinhibitedMDA-MB-231xenografttumorgrowthinadose-dependentmannerwithnon-toxicity.SignificantlyloweredKi-67(aproliferationmarker)andCD31expression.SuccessfullysuppressedtheexpressionofHIF-1αandVEGFintumortissues.REFERENCES[1].KimDH,etal.HS-1793,aresveratrolanalogue,downregulatestheexpressionofhypoxia-inducedHIF-1andVEGFandinhibitstumorgrowthofhumanbreastcancercellsinanudemousexenograftmodel.IntJOncol.2017Aug;51(2):715-723.[2].KimDH,etal.Resveratrolanalogue,HS-1793,inducesapoptoticcelldeathandcellcyclearrestthroughdownregulationofAKTinhumancoloncancercells.OncolRep.2017Jan;37(1):281-288.MceP