SETDB1-TTD-IN-1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESETDB1-TTD-IN-1Cat.No.:HY-141539CASNo.:2755823-12-0分⼦式:C₂₈H₃₁N₅O₂分⼦量:469.58作⽤靶点:HistoneMethyltransferase作⽤通路:Epigenetics储存⽅式:4°C,protectfromlight,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light,storedundernitrogen)溶解性数据体外实验DMSO:125mg/mL(266.20mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1296mL10.6478mL21.2956mL5mM0.4259mL2.1296mL4.2591mL10mM0.2130mL1.0648mL2.1296mL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SETDB1-TTD-IN-1⼀种有效，选择性和内性结合剂竞争性的SETDB1-TTD抑制剂，Kd值为88nM。SETDB1-TTD-IN-1可⽤于SETDB1-TTD关联的⽣物学功能和疾病的研究。IC50&TargetKd:88nM(SETDB1-TTD)[1]体外研究SETDB1-TTD-IN-1showssomeactivityfor53BP1andJMJD2A,withKdsof4.3μMand86μM,respectively.1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESETDB1-TTD-IN-1doesnotshowactivityagainst14ofthe16testedtudordomains(Kd>100μM)[1].SETDB1-TTD-IN-1(2.5-40μM)efficientlyanddose-dependentlystabilizestheSETDB1-TTDproteininHEK293Tcells[1].SETDB1-TTD-IN-1(2.5-40μM;24h)significantlyaffectedtheexpressionof72genesinhumanacutemonocyticleukemiaTHP-1cells[1].REFERENCES[1].GuoY,et,al.Structure-GuidedDiscoveryofaPotentandSelectiveCell-ActiveInhibitorofSETDB1TudorDomain.AngewChemIntEdEngl.2021Apr12;60(16):8760-8765.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;021-589