SIM1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESIM1Cat.No.:HY-141438分⼦式:C₇₉H₉₈Cl₂N₁₄O₁₃S₃分⼦量:1618.81作⽤靶点:PROTACs;EpigeneticReaderDomain作⽤通路:PROTAC;Epigenetics储存⽅式:-20°C,protectfromlight,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light,storedundernitrogen)溶解性数据体外实验DMSO:100mg/mL(61.77mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM0.6177mL3.0887mL6.1774mL5mM0.1235mL0.6177mL1.2355mL10mM0.0618mL0.3089mL0.6177mL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(protectfromlight,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SIM1⼀种有效的vonHippel-Lindau(VHL)-basedPROTAC，能够对所有BET家族成员进⾏降解，并优先降解BRD2(IC50=1.1nM;Kd=186nM)。SIM1显⽰出持续的抗癌活性[1]。IC50&TargetBRD2BRD2BRD3BRD41.1nM(IC50)186nM(Kd)体外研究SIM1(1nM;30hours;MV4-11cells)resultsinmeasurablecellulardeathafter6hours[1].SIM1(1µM;4hours;HEK293cells)degradesBETproteins[1].1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESIM1inducesconformationalchangesuponbindingtotheBETproteintosimultaneouslyengagewithhighaviditybothitsbromodomainsinacisintramolecularfashion.SIM1engagesBD1andBD2intramolecularlyandformsa1:1:1ternarycomplexwithVHLandBRD4[1].CellViabilityAssay[1]CellLine:MV4-11cellsConcentration:1nMIncubationTime:30hoursResult:Resultedinmeasurablecellulardeathafter6hours.WesternBlotAnalysis[1]CellLine:HEK293cellsConcentration:1µMIncubationTime:4hoursResult:DegradedBETproteins.REFERENCES[1].SatomiImaide,etal.TrivalentPROTACsenhanceproteindegradationthroughcooperativityandavidity.BiologicalandMedicinalChemistry.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3