SE-7552-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESE-7552Cat.No.:HY-161305CASNo.:2243575-79-1分⼦式:C₁₅H₁₂F₃N₅O分⼦量:335.28作⽤靶点:HDAC作⽤通路:CellCycle/DNADamage;Epigenetics储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性SE-75522-(difluoromethyl)-1,3,4-oxadiazole(DFMO)衍⽣物，⼀种具有⼝服活性的、⾼选择性、⾮异羟肟酸HDAC6抑制剂，IC50为33nM。SE-7552的选择性⽐所有其他已知的HDAC同⼯酶⾼850倍。SE-7552能够阻断体内多发性⾻髓瘤的⽣长。SE-7552在饮⾷诱导的肥胖⼩⿏中充当抗肥胖剂。IC50&TargetHDAC633nM(IC50)体内研究SE-7552(30mg/kg;asingleoraldose)increasesthelevelsofacetylatedα-tubulinforover24hoursinmice.SE-7552hasnoeffectontheacetylationofH3(abiomarkerforinhibitionofClassIHDACs)[1].SE-7552(10mg/kg;orally;daily)combinatedwithPomalidomide(HY-10984;1mg/kg;IPdaily)significantlydelaystumorgrowthincomparisontoPomalidomidealone,aswellasenhancedthesurvivalofthemicewithhumanH929MMcells[1].SE-7552demonstratedsuperiorPK,withamaximumexposureof597ng/mlandahalf-lifeof7.2hoursafterasingleoraldoseof5mg/kginthemouse[1].REFERENCES[1].JasonAHolt,etal.SE-7552,aHighlySelective,Non-HydroxamateInhibitorofHistoneDeacetylase-6BlocksMultipleMyelomaGrowthInVivo.Blood(2018)132(Supplement1):3215.[2].BeateKönig,etal.2-(Difluoromethyl)-1,3,4-oxadiazoles:TheFutureofSelectiveHistoneDeacetylase6Modulation?ACSPharmacol.Transl.Sci.2024,February20.McePdfHeight1/1MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;021-58955