LSD1-IN-46-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemELSD1-IN-46Cat.No.:HY-179339CASNo.:2982716-97-0分⼦式:C₂₂H₂₉N₃O分⼦量:351.49作⽤靶点:HistoneDemethylase作⽤通路:Epigenetics储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性LSD1-IN-46⼀种强效且具有⼝服活性的赖氨酸特异性去甲化酶1(LSD1)抑制剂，IC50值为0.082μM。LSD1-IN-46可阻断β-catenin介导的转录程序，从⽽抑制胃癌细胞的⼲性。LSD1-IN-46具有显著的抗肿瘤活性，可⽤于胃癌的研究。IC50&TargetLSD10.082μM(IC50)体外研究LSD1-IN-46(CompoundX-1)(0.5-2μM;5days)increasesH3K4me1/2levelsinMKN-45cellsandthiseffectisabsentinLSD1-KOcells[1].LSD1-IN-46(0.5-2μM;5days)inhibitsself-renewal,sphereformationandcolonyformationofMKN-45cells,anddownregulatestheexpressionofβ-catenin,c-MycandstemnessmarkersOCT4,NANOG,SOX2[1].WesternBlotAnalysis[1]CellLine:MKN-45Concentration:0.5,1,2μMIncubationTime:5daysResult:DecreasedOCT4,NANOG,andSOX2levles.Downregulatedtheexpressionofβ-catenin,c-Myc.1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE体内研究LSD1-IN-46(CompoundX-1)(10-20mg/kg;i.g.;Oncedaily;oncedailyfor11days)reducestumorsizeandweightinsubcutaneousinjectionofMFCgastriccancercellsinBALB/cnude[1].AnimalModel:BALB/cnudemicewithinjectionofMFCgastriccancercells(male,6-8weeksold)[1]Dosage:10,20mg/kgAdministration:Oralgavage;Oncedaily;11daysResult:Reducedtumorsizeandweight.Didnotaffectmousebodyweightorcausingobvioushepatorenaltoxicity.Downregulatedtheexpressionofβ-catenin,c-Myc,SOX2,NANOGintumortissues.REFERENCES[1].DaiXJ,etal.IdentificationofNovelPhenoxazine-DerivedLSD1InhibitorsSuppressingGastricCancerStemnessbyβ-CateninTranscriptionalRegulation.JMedChem.2025;68(21):22896-22917.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-37