LD5097-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemELD5097Cat.No.:HY-179234分⼦式:C₇₄H₇₅F₄N₁₃O₈S分⼦量:1382.53作⽤靶点:PROTACs;RIPkinase;Apoptosis;Caspase;PARP作⽤通路:PROTAC;Apoptosis;CellCycle/DNADamage;Epigenetics储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性LD5097⼀种⾼效且选择性的PROTAC降解剂，靶向RIPK1。LD5097可快速有效地下调RIPK1，并显著增强Jurkat细胞中TNFα介导的细胞凋亡(apoptosis)。LD5097可显著提⾼裂解型caspase-3/7和PARP的⽔平。LD5097可⽤于急性T淋巴细胞⽩⾎病的研究[1]。IC50&TargetCaspase-3Caspase-7体外研究LD5097(Compound24b)(24h)exhibitspotentRIPK1(DC50=0.7nM)degradationactivityinJurkatnLuc-RIPK1cells[1].LD5097(1.6-1000nM,24h)resultsinadose-dependentdegradationofendogenousRIPK1after24h(DC50=2.6nM)inJurkatcells[1].LD5097exhibitspotentdegradationofendogenousRIPK1,withDC50valuesof2.8and0.8nMinbothMOLM14andU937cells,respectively[1].LD5097(100nM,0.5-24h)cancompletelydegradeRIPK1inJurkatcellswithin2hours[1].LD5097's(100nM,24h)degradationabilitydependsonabifunctionalPROTACmechanism,whichrequiressimultaneousbindingtoRIPK1andVHLE3ligases[1].LD5097(100nM,72h)enhancesTNFα-mediatedapoptosisinJurkatcells[1].LD5097(0-10μM,24h)achievescompletedegradationofRIPK1at100nMinRamoscellsbutfailstodosoevenat10μMinA20cells[1].WesternBlotAnalysis[1]CellLine:JurkatcellsConcentration:100nM1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEIncubationTime:0.5h,1h,2h,4h,6h,12h,24hResult:CompletelydegradedRIPK1inJurkatcellswithin2hours.ApoptosisAnalysis[1]CellLine:JurkatcellsConcentration:100nMIncubationTime:72hResult:CombinedwithTNFαsignificantlyinducedapoptosis.Cleavedcaspase-3/7andPARPlevelsincreased.ApoptosiscouldbereversedbyZ-VAD-FMK(HY-16658B).WesternBlotAnalysis[1]CellLine:Ramoscells,A20cellsConcentration:0μM,0.1μM,1μM,10μMIncubationTime:24hResult:CompletedegradationofRIPK1at100nMinRamoscells,butfailedtodosoevenat10μMinA20cells.体内研究LD5097(Compound24b)(10mg/kg,i.v.,once)significantlydegradesRIPK1inJurkatcellxenograftmicetumor[1].AnimalModel:6-week-oldfemalenudemiceweresubcutaneouslyinjectedwith2.5×106Jurkatcellssuspendedina1:1mixturewithMatrigel[1].Dosage:10mg/kgAdministration:I.v.,onceResult:Inducedadecreaseofmorethan70%inRIPK1proteinlevelsintumortissueatboth6and24hoursafteradministration.REFERENCES[1].LuD,etal.Design,Optimization,andDevelopmentofRIPK1DegraderswithImprovedPharmacokineticandPharmacodynamicProperties.JMedChem.2025Nov13;68(21):22246-22263.McePdfHeight2/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasnotbeenfullyvalidatedformedical