PRMT5-IN-1-hydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPRMT5-IN-1hydrochlorideCat.No.:HY-126256A分?式:C??H??Cl?N?O?分?量:455.29作?靶點:HistoneMethyltransferase作?通路:Epigenetics儲存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)BIOLOGICALACTIVITY?物活性PRMT5IN-1hydrochloride(compound9)?種半縮醛胺，?種有效的選擇性蛋?精氨酸甲轉(zhuǎn)移酶5(PRMT5)抑制劑，抑制PRMT5/MEP50的IC50值為11nM。PRMT5IN-1hydrochloride在?理條件下可以轉(zhuǎn)化為醛并與C449反應(yīng)形成共價加合物。IC50&TargetIC50:11nM(PRMT5/MEP50)[1]體外研究PRMT5IN-1(compound9;0-500nM)hydrochlorideinhibitsthePRMT5/MEP50complex[Kinact/KI=1.2×105M-1min-1]veryrapidlywithaKinactof0.068min-1andagoodbindingaffinity(KI=55nM)[1].PRMT5IN-1(0-1000nM;3d;Granta-519cells)hydrochlorideinhibitstheexpressionofcellularsDMAwithanIC50valueof0.012μM[1].PRMT5IN-1(0-1μM;10d;Granta-519cells)hydrochlorideinhibitscellproliferationinadose-dependentmannerwithanIC50valueof0.06μM[1].CellViabilityAssay[1]CellLine:Granta-519cellsConcentration:0,0.0001524,0.000457,0.001372,0.004115,0.012346,0.037037,0.111111,0.333333and1μMIncubationTime:10daysResult:Inhibitedcellproliferative,inwhichcellsdiedonday10athighconcentrations(0.3and1μM).WesternBlotAnalysis[1]1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECellLine:Granta-519cellsConcentration:0,0.05,0.15,0.46,1.37,4,12,37,111,333,1000nMIncubationTime:3daysResult:InhibitedcellularsDMAinGranta-519cellsinadose-dependentmanner.REFERENCES[1].LinH,et,al.DiscoveryofPotentandSelectiveCovalentProteinArginineMethyltransferase5(PRMT5)Inhibitors.ACSMedChemLett.2019May22;10(7):1033-1038.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792