COX-2-IN-59-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECOX-2-IN-59Cat.No.:HY-179125分⼦式:C₁₈H₁₉N₃O₆S分⼦量:405.42作⽤靶点:COX;Bcl-2Family;Caspase;Apoptosis作⽤通路:Immunology/Inflammation;Apoptosis储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性COX-2-IN-59⼀种⾼效且选择性的COX-2抑制剂，IC50值为0.052μM。COX-2-IN-59对COX-2的选择性对COX-1的200倍以上(对COX-1的IC50值为11.16μM)。COX-2-IN-59能够降低COX-2⽔平，诱导细胞周期阻滞，并通过上调Bax表达、下调Bcl-2⽔平以及激活caspase-3来触发细胞凋亡(apoptosis)。COX-2-IN-59可⽤于结肠癌的相关研究[1]。IC50&TargetCOX-2COX-10.052μM(IC50)11.16μM(IC50)体外研究COX-2-IN-59(compound5d)(12.5-100μM;24h)inhibitsA-549,HOS,MCF‐7,HT‐29,PC3,andCaco‐2cellgrowthwithIC50sof4,67.3,30.5,8.5,29.1,and2.6μM,respectively[1].COX-2-IN-59(2.6μM;24h)inducesG1/Scellcyclearrest,andtriggersapoptosisinCaco-2cellsbyincreasingBaxexpression,decreasingBcl-2levels,andactivatingcaspase-3[1].COX-2-IN-59(2.6μM;24h)significantlyreducesCOX-2levelsto3.858ng/mL(0.494‐foldrelativetocontrol)inCaco-2cells[1].CellViabilityAssay[1]CellLine:A-549,HOS,MCF-7,HT-29,PC3,andCaco-2cellsConcentration:12.5-100μMIncubationTime:24hResult:InhibitedA-549,HOS,MCF-7,HT-29,PC3,andCaco-2cellgrowthwithIC50sof4,67.3,30.5,8.5,29.1,and2.6μM,respectively.1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEApoptosisAnalysis[1]CellLine:Caco-2Concentration:2.6μMIncubationTime:24hResult:DemonstratedpotentproapoptoticactivityinCaco-2cells,inducinganearlyeightfoldincreaseintotalapoptosis(24.38%vs.3.16%incontrols).Inducedadramatic63-foldincrease(15.86%vs.0.25%)inlateapoptosis,andan11-foldincrease(4.85%vs.0.42%)inearlyapoptosis.CellCycleAnalysis[1]CellLine:Caco-2Concentration:2.6μMIncubationTime:24hResult:ShowedadramaticdecreaseinG2/Mphasecellsinthetreatedgroup(3.82%)comparedtothecontrolgroup(22.05%).SignificantlyincreasedcellsintheG0/G1phase(64.06%vs.48.29%incontrol).InducedG1/Sphasecellcyclearrest.WesternBlotAnalysis[1]CellLine:Caco-2Concentration:2.6μMIncubationTime:24hResult:Ineaingtothanreioxpesionfleas‐3re.ssingtheexpressionofBcl‐2,ultimatelyELISAAssay[1]CellLine:Caco-2Concentration:2.6μMIncubationTime:24hResult:SignificantlyreducedCOX-2levelsto3.858ng/mL(0.494‐foldrelativetocontrol).REFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].KassemAF,etal.DualAnticancerandCOX-2InhibitoryActivityofTailoredParacetamol-AlkanesulfonateConjugates:APromisingTherapeuticApproach.ArchPharm(Weinheim).2025;358(10):e70125.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalappl