dFKBP-1-DataSheet-生命科学试剂-MedChemExpressVIP

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEdFKBP-1Cat.No.:HY-103634CASNo.:1799711-22-0分⼦式:C₅₃H₆₄N₆O₁₄分⼦量:1009.11作⽤靶点:PROTACs;FKBP作⽤通路:PROTAC;Apoptosis;Autophagy;Immunology/Inflammation储存⽅式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性数据体外实验DMSO:100mg/mL(99.10mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM0.9910mL4.9549mL9.9097mL5mM0.1982mL0.9910mL1.9819mL10mM0.0991mL0.4955mL0.9910mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(storedundernitrogen)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。BIOLOGICALACTIVITY⽣物活性dFKBP-1⼀种于PROTAC的有效的FKBP12降解剂。dFKBP-1包含FKBP12配体SLF(HY-114872)，于Thalidomide的Cereblon配体和⼀个linker。IC50&TargetCereblonFKBP体外研究dFKBP-1potentlydecreasesFKBP12abundanceinMV4;11cells,leadingtoover80%reductionofFKBP12at0.1μMand50%reductionat0.01μM.AswithdBET1,destabilizationofFKBP12bydFKBP-1isrescued1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEbypre-treatmentwithCarfilzomib,MLN4924,freeSLForfreeThalidomide.Cereblon(CRBN)-dependentdegradationisestablishedusingpreviouslypublishedisogenic293FTcelllineswhicharewild-type(293FT-WT)ordeficient(293FT-CRBN−/−)forCRBN.Treatmentof293FT-WTcellswithdFKBP-1inducespotent,dose-dependentdegradationofFKBP12,whereas293FT-CRBN−/−areunaffected[1].REFERENCES[1].WinterGE,etal.DRUGDEVELOPMENT.Phthalimideconjugationasastrategyforinvivotargetproteindegradation.Science.2015Jun19;348(6241):1376-81.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;021