Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEdFKBP-1Cat.No.:HY-103634CASNo.:1799711-22-0分?式:C??H??N?O??分?量:1009.11作?靶點(diǎn):PROTACs;FKBP作?通路:PROTAC;Apoptosis;Autophagy;Immunology/Inflammation儲(chǔ)存?式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(99.10mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM0.9910mL4.9549mL9.9097mL5mM0.1982mL0.9910mL1.9819mL10mM0.0991mL0.4955mL0.9910mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(storedundernitrogen)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。BIOLOGICALACTIVITY?物活性dFKBP-1?種于PROTAC的有效的FKBP12降解劑。dFKBP-1包含F(xiàn)KBP12配體SLF(HY-114872)，于Thalidomide的Cereblon配體和?個(gè)linker。IC50&TargetCereblonFKBP體外研究dFKBP-1potentlydecreasesFKBP12abundanceinMV4;11cells,leadingtoover80%reductionofFKBP12at0.1μMand50%reductionat0.01μM.AswithdBET1,destabilizationofFKBP12bydFKBP-1isrescued1/2MasterofBioactiveMolecules—您?邊的抑制劑?師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