Anticancer-agent-205-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAnticanceragent205Cat.No.:HY-162456分⼦式:C₅₂H₆₀I₂N₄分⼦量:994.87作⽤靶点:Apoptosis;ReactiveOxygenSpecies作⽤通路:Apoptosis;Immunology/Inflammation;MetabolicEnzyme/Protease;NF-κB储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Anticanceragent205(compound9)⼀种有效的抗癌剂。Anticanceragent205与G4-mtDNA靶标结合并抑制mtDNA(线粒体因组)的复制、转录和翻译。Anticanceragent205会导致线粒体功能障碍、增加ROS产⽣、诱导DNA损伤和细胞衰⽼。Anticanceragent205诱导细胞凋亡(apoptosis)和细胞周期停滞在G0/G1期。Anticanceragent205具有研究结直肠癌的潜⼒[1]。体外研究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—您⾝边的抑制剂⼤师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%.体内研究Anticanceragent205(5mg/kg;i.v.;every2daysfor16days)inhibitstumorgrowthinxenograftmousemodelofHCT116[1].AnimalModel:maleBalb/cnudemice(HCT116cells)[1].Dosage:5mg/kgAdministration:I.v.;every2daysfor16daysResult:Significantlyinhibitedthegrowthoftumorswiththetumorgrowthreducedby70%approximately.REFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].ZhengBX,etal.Mitochondria-SelectiveDicationicSmall-MoleculeLigandTargetingG-QuadruplexStructuresforHumanColorectalCancerTherapy.JMedChem.2024Apr25;67(8):6292-6312.McePdfHeightCaution:Producthasnotbeenfullyvalidatedfor