PRMT5-IN-19-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPRMT5-IN-19Cat.No.:HY-149005分?式:C??H??N?O分?量:396.48作?靶點(diǎn):HistoneMethyltransferase作?通路:Epigenetics儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物PRMT5-IN-19(Compound41)?種具有?服活性的?核苷PRMT5選擇性抑制劑，IC50值為23.9nM(radioactivebiochemicalassay),4活性中的SAM-bindingpocket并封閉甲轉(zhuǎn)移酶的活性，選擇性優(yōu)于PRMTs和PKMTs。PRMT5-IN-19通過誘導(dǎo)細(xì)胞凋亡(apoptosis)來抑制細(xì)IC50&PRMT5PRMT1PRMTarget23.9nM(IC50)3.252μM(IC50)>20μ體外PRMT5-IN-19(Compound41,5days)hasstronganti-proliferativeeffectsagainsttheA375cellwithanIC50valueof1.36μM[1].研究PRMT5-IN-19showshigherselectivityforPRMT5(IC50valueof23.9nM)thanotherhistonemethyltransferases(PRMT1andPRMT4),PRMT5-IN-19bindswiththeSAM-bindingpocketinPRMT5[1].PRMT5-IN-19(4-5days)Inhibitsproliferationofmultiplecancercelllines(A-375,CHL-1,SNU-423,SNU-449,MDA-MB-231,MDA-MA-41.08to3.45μM[1].PRMT5-IN-19inhibitsargininesymmetricaldimethylationinA375cells[1].PRMT5-IN-19(0-4μM,48h)suppressesA375cellproliferationbyinducingapoptosisinaconcentration-dependentmanner[1].CellProliferationAssay[1]CellLine:A-375,CHL-1,SNU-423,SNU-449,MDA-MB-231,MDA-MA-453,MV-4-11,MOLM13Concentration:0-10μMIncubationTime:5daysResult:InhibitedproliferationofmultiplecancercelllineswithIC50valuerangingfrom1.08to3.45μM.WesternBlotAnalysis[1]1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECellLine:A-375cellsConcentration:0.5,1,2,4,8μMIncubationTime:48h.Result:Inhibitedargininesymmetricaldimethylationinadose-dependentmanner.體內(nèi)研PRMT5-IN-19(Compound41,A375xenograftmodel,75mg/kg/d,p.o.,19days)hasgoodPKpropertiesandsignificantantitumorefficac究toxicity[1].AnimalModel:A375cell-derivednudemousexenograftmodel[1].Dosage:75mg/kg/dAdministration:P.o.,19daysResult:Hadnoeffectonthebodyweight,displayedantitumorefficacywithatumorgrowthinhibition(TGI)rateof73%byinhAnimalModel:Ratsandmice[1].Dosage:10mg/kgforp.o.,3mg/kgfori.vAdministration:P.o.,i.v.(PharmacokineticAnalysis)Result:PharmacokineticparametersforREFERENCESPRMT5-IN-19inSDRatsandMicea,c[1].speciesPRMT5-IN-[1].DeqinRong,etal.Structure-AidedDesign,Synthesis,andBiologicalEvaluationofPTargetingProteinArginineMethyltransferase5.JMedChem.202219T1/2(h)CmaxMcePdfHeight(ng/mL)CL(mL/min/kg)F(%)rativ(3mg/kg)/td>2.58310po(10mg/kg)/td>7.518.227.25po(10mg/kg)/td>2.9527.723.7mouseiv(3mg/kg)/td>4.711532/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEpo(10mg/kg)/td>128Caution:Producthasnotbeenfullyvalidatedformedicalappli