Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAnticanceragent205Cat.No.:HY-162456分?式:C??H??I?N?分?量:994.87作?靶點(diǎn):Apoptosis;ReactiveOxygenSpecies作?通路:Apoptosis;Immunology/Inflammation;MetabolicEnzyme/Protease;NF-κB儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Anticanceragent205(compound9)?種有效的抗癌劑。Anticanceragent205與G4-mtDNA靶標(biāo)結(jié)合并抑制mtDNA(線粒體因組)的復(fù)制、轉(zhuǎn)錄和翻譯。Anticanceragent205會(huì)導(dǎo)致線粒體功能障礙、增加ROS產(chǎn)?、誘導(dǎo)DNA損傷和細(xì)胞衰?。Anticanceragent205誘導(dǎo)細(xì)胞凋亡(apoptosis)和細(xì)胞周期停滯在G0/G1期。Anticanceragent205具有研究結(jié)直腸癌的潛?[1]。體外研究Anticanceragent205(compound9)(4μM;1h)interactswithG4-mtDNAinHCT116cells[1].Anticanceragent205(0,1,2,4μM;48h)reducesthemRNAlevelofND2andND5inHCT116,HFF1cells[1].Anticanceragent205(0,1,2,4μM;48h)reducestheproteinlevelsofND3,ND4,ND6,COX1,COX2,COX3,CYTB,ATP6,andATP8inHCT116cells[1].Anticanceragent205(0-4μM)increasestheROSlevelinaconcentration-dependentmanner[1].Anticanceragent205(0-4μM;72h)inducesDNAdamageandcellularsenescence[1].CellCytotoxicityAssay[1]CellLine:HCT116,LoVo,HeLa,HepG2,PANC-1,MDA-MB-231,HFF1,BJcellsConcentration:0-40μMIncubationTime:48hResult:ShowedcytotoxicityforHCT116,LoVo,HeLa,HepG2,PANC-1,MDA-MB-231,HFF1,BJcellswithIC50sof3.4,13.4,23.5,>40,24.8,34.6,32.7,>40μM,respectively.RT-PCR[1]1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECellLine:HCT116,HFF1cellsConcentration:0,1,2,4μMIncubationTime:48hResult:CausedasignificantreductionofmRNAlevelsforND1,ND2,ND3,ND4,ND4L,ND5,COX2,ATP6,andATP8inHCT116,onlyND2andND5showedasignificantreductioninHFF1cells.WesternBlotAnalysis[1]CellLine:HCT116cellsConcentration:0,1,2,4μMIncubationTime:48hResult:ShowedthattheproteinlevelsofND3,ND4,ND6,COX1,COX2,COX3,CYTB,ATP6,andATP8weredecreasedmarkedly.CellCycleAnalysis[1]CellLine:HCT116cellsConcentration:0,1,2,4μMIncubationTime:48hResult:InducedcellcyclearrestedintheG0/G1phasewithThepercentageoftheG0/G1phaseisincreasedfrom50.66to66.01%,inaconcentration-dependentmanner,inducesapoptosisbyincreasestheexpressionofcleaved-caspase3andtheapoptosiscellincreasedfrom2.64%to27.4%.體內(nèi)研究Anticanceragent205(5mg/kg;i.v.;every2daysfor16days)inhibitstumorgrowthinxenograftmousemodelofHCT116[1].AnimalModel:maleBalb/cnudemice(HCT116cells)[1].Dosage:5mg/kgAdministration:I.v.;every2daysfor16daysResult:Significantlyinhibitedthegrowthoftumorswiththetumorgrowthreducedby70%approximately.REFERENCES2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[1].ZhengBX,etal.Mitochondria-SelectiveDicationicSmall-MoleculeLigandTargetingG-QuadruplexStructuresforHumanColorectalCancerTherapy.JMedChem.2024Apr25;67(8):6292-6312.McePdfHeightCaution:Producthasnotbeenfullyvalidatedfor