β-carboline-ACS81-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEβ-carboline-ACS81Cat.No.:HY-179399分⼦式:C₂₆H₂₇N₃O₂S₂分⼦量:477.64作⽤靶点:Apoptosis;MitochondrialMetabolism作⽤通路:Apoptosis;MetabolicEnzyme/Protease储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性β-carboline-ACS81⼀种具有强效抗肿瘤特性的β-carboline衍⽣物。β-carboline-ACS81通过线粒体膜电位崩溃诱导HL-60细胞凋亡(apoptosis)，并使细胞周期阻滞于G2/M期。β-carboline-ACS81对HL-60细胞具有显著的抗增殖活性(IC50=1.52μM)。β-carboline-ACS81可⽤于⽩⾎病、组织细胞淋巴瘤、肝细胞癌、恶性⿊⾊素瘤、结直肠癌和肺癌的研究[1]。体外研究β-carboline-ACS81(Compound12c)(72h)exhibitssignificantanti-proliferativeactivityagainsttumorcelllines,withIC50valuesof1.52,2.03,2.8,6.04,and6.57,37.23μMforHL-60,U937,HepG2,HCT-116,A375andA549respectively,comparedwithanIC50valueof33.92μMinnormalL-02cells[1].β-carboline-ACS81(0.38-1.52μM,48h)inducesG2/Mphasearrest,therebyinhibitingcellproliferation,andapoptosisinHL-60cells,withthelatterpotentiallymediatedbymitochondrialpathwayinvolvementasevidencedbydiminishedmitochondrialmembranepotential[1].CellCycleAnalysis[1]CellLine:HL-60cellsConcentration:0.38,0.76and1.52μMIncubationTime:48hResult:InducedagradualincreaseintheproportionofcellsintheG2/Mphasewiththerisingconcentrations.ElevatedG2/Mphasecellpercentagefrom18.75%intheblankcontrolgroupto20.58%,25.63%,andultimatelyto31.28%.CausedacontinuousdecreaseinthenumberofcellsintheG1phase,whichdropped1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEfrom65.97%intheblankcontrolgroupto61.82%,58.39%,and50.82%,respectively.InducedlittleeffectonthenumberofcellsintheSphase,whichremainedlargelyunchanged.ApoptosisAnalysis[1]CellLine:HL-60cellsConcentration:0.38,0.76and1.52μMIncubationTime:48hResult:Inducedprogressivechromatincondensationandcellmembranedisruptionincorrelationwiththeconcentration.Preservednormalnuclearmorphologyinmostcellsbutinducedincreasedfluorescence(earlychromatincondensation)insomecellsat0.38μM.Inducedintensenuclearfluorescence(pyknosis)innumerouscellsandclearnuclearfragmentationintovariablebrightblueparticles(apoptoticbodies)at0.76μM.Eliminatednormalnuclearmorphology,withmostcellsshowingadvancednuclearpyknosisandkaryorrhexisthatformeddense,intenselyfluorescentbluegranularaggregatesat1.52μM.Causedadose-dependentincreaseinapoptoticcellsto14.73%,27.68%,and40.89%atescalatingconcentrations.REFERENCES[1].HuX,etal.Enhancementofanticancerpotentialofnovelβ-carbolinederivativesbyACS81hybridization.BioorgMedChemLett.2026Feb1;131:130440.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalap