CDK2-IN-51-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECDK2-IN-51Cat.No.:HY-180157CASNo.:1443-10-3分⼦式:C₁₈H₁₆N₄分⼦量:288.35作⽤靶点:CDK作⽤通路:CellCycle/DNADamage储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性CDK2-IN-51⼀种吡唑并吡啶衍⽣物，⼀种CDK2抑制剂，其IC50为23.47nM。CDK2-IN-51导致DNA复制因⼦(Polα、MCM7、ORC2和ORC4)表达减少和G1期前细胞周期阻滞。CDK2-IN-51不具有促凋亡作⽤，且对CDK2蛋⽩表达的响不显著。CDK2-IN-51可⽤于结直肠癌的研究。IC50&TargetCDK2CDK223.47nM(IC50)4.11μM(Ki)体外研究CDK2-IN-51(compound6)(10-50μM;24-72h)demonstratessignificantantiproliferativeactivityagainstHCT-116andHT-29cellswithnocytotoxicitytoNCM-460Dcells[1].CDK2-IN-51(40-50μM;48h)inducespre-G1phasearrestinHCT-116andHT-29cellswithoutS-phasearrest[1].CDK2-IN-51(40-50μM;48-72h)downregulatesCDK2proteintargetsinvolvedinDNAreplicationprocess;Polα,MCM7,ORC2,andORC4inHCT-116andHT-29cells,anddoesnothaveapro-apoptoticeffectandhadnosignificanteffectonCDK2proteinexpression[1].CellViabilityAssay[1]CellLine:HCT-116,HT-29,NCM-460DConcentration:10μM,20μM,40μM,50μMIncubationTime:24h,48h,72hResult:At72h,exhibitedsignificantantiproliferativeeffectsonHCT-116andHT-29cells,with1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEIC50valuesof46.41μMand61.47μM,respectively,andshowednocytotoxicityonNCM-460Dcells,withanIC50valueof>100μM.CellCycleAnalysis[1]CellLine:HCT-116,HT-29Concentration:40μM,50μMIncubationTime:48hResult:Causedasignificantincreaseinthepre-G1phasepopulationinbothHCT-116andHT-29cells,indicatingcelldeath,andnoS-phasearrestwasobserved,suggestingthatthecompounddidnotinduceapoptosis.WesternBlotAnalysis[1]CellLine:HCT-116,HT-29Concentration:40μM,50μMIncubationTime:48h,72hResult:ReducedtheexpressionofCDK2targets,MCM7,ORC2,andORC4proteins.ReducedPolαlevels.REFERENCES[1].IssaDAE,etal.Design,synthesisandmoleculardockingofPyrazolo[3,4-b]pyridinederivativesaspotentialCDK2pathwayinhibitorsincolorectalcancercells.BioorgChem.2025Dec3:168:109335.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuse