Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemEPROTACHDACdegrader-2Cat.No.:HY-174444分子式:C??H??N?O?分子量:733.81作用靶點:PROTACs;HDAC作用通路:PROTAC;CellCycle/DNADamage;Epigenetics儲存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性PROTACHDACdegrader-2是IIb類HDACs的選擇性PROTAC降解劑，其對HDAC6和HDAC10的DC50值分別為13nM和29nM。PROTACHDACdegrader-2對血液和實體瘤細胞系表現(xiàn)出低細胞毒性。PROTACHDACdegrader-2可用于IIb類HDACs的化學敲低。(粉色：HDAC6/10配體(HY-174471)，藍色：E3連接酶CRBN配體(HY-131717)，E3連接酶配體-連接子偶聯(lián)物:HY-174473[1]。IC50&TargethHDAC6hHDAC10Cereblon13nM(DC50)29nM(DC50)體外研究PROTACHDACdegrader-2(CompoundAP1)(90min)demonstratesinhibitoryactivityagainstHDAC6andHDAC10,withIC50valuesof0.04μMand0.022μMinfluorogenicenzymeinhibitionassaysusingZ-Lys(Ac)-AMCorAc-spermidine-AMCassubstrates[1].PROTACHDACdegrader-2(50-1000nM,0-1440min)showsstabilitycomparabletoTubastatinA(HY-13271A)inhumanplasma[1].PROTACHDACdegrader-2(1-5μM,24h)showsproteasome-dependentandlong-lastingdegradationeffectoftheHDAC6andHDAC10inMM.1ScellsanddegradesHDAC6andHDAC10inMCF-7cells[1].PROTACHDACdegrader-2(1μM,24h)causesnorelevantHDAC1,HDAC4,HDAC7orHDAC8degradationinMM.1Scells[1].PROTACHDACdegrader-2(1μM,24h)inducesupregulationofAc-α-tubulin,aknownsubstrateofHDAC6,comparabletoVorinostat(HY-10221)[1].PROTACHDACdegrader-2(1-5μM,6-24h)inducesneosubstratedegradationoccursviaCRBNandnotHDACengagementinMM.1Scells[1].PROTACHDACdegrader-2(10μM,48h)inducesasignificantprolongationoftheG1-phaseinMM.1Scells[1].1/2 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEPROTACHDACdegrader-2(1-5μM,24h)doesnotaffecttheLC3-IandLC3-IIlevelsinMM.1Scells[1].PROTACHDACdegrader-2(10μM,24h)attenuatescellmigrationsignificantlyinMDA-MB-231cells[1].WesternBlotAnalysis[1]CellLine:MM.1ScellsConcentration:1μMIncubationTime:6hafterTubastatinA(HY-13271A)(10μM),Pomalidomide(HY-10984)(10μM)orPevonedistat(MLN4924)(HY-70062)(10μM)treatedfor0.5hResult:InducedsignificantdegradationofHDAC6andHDAC10aloneandrecoveredthelevelsofHDAC6andHDAC10forthegroupswithpretreatments.RecoveredthelevelsofIKZF1forthegroupspretreatedwithMLN4924butnotTubastatinA.WesternBlotAnalysis[1]CellLine:MM.1ScellsConcentration:5μMIncubationTime:24hResult:DegradedIKZF1andIKZF3stronglyandreducedGSPT1levelsslightly.REFERENCESZhaiS,etal.DevelopmentandCharacterizationoftheFirstSelectiveClassIIbHistoneDeacetylaseDegraders.JMedChem.2025Jul10;68(13):13793-13821.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalappl