Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemESJL2-1Cat.No.:HY-174908分?式:C??H??N?O分?量:334.45作?靶點(diǎn):HistoneMethyltransferase;11β-HSD;AndrogenReceptor作?通路:Epigenetics;MetabolicEnzyme/Protease;VitaminDRelated/NuclearReceptor儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性SJL2-1?種PRMT5抑制劑，其IC50值為1.56μM。SJL2-1能抑制前列腺癌細(xì)胞的增殖、遷移和侵襲能?，促進(jìn)細(xì)胞凋亡(apotosis)并使細(xì)胞周期阻滯于G0/G1期。SJL2-1可靶向細(xì)胞內(nèi)的PRMT5結(jié)合，抑制雄激素受體的甲化及其表達(dá)。SJL2-1可?于早期雄激素敏感性前列腺癌和晚期去勢(shì)抵抗性前列腺癌(CRPC)的相關(guān)研究[1]。體外研究SJL2-1(2.96-60μM,24-96h)suppressesproliferation,migration,andinvasioninprostatecancercellsincluding22RV1,PC-3,andLNCaPcells[1].SJL2-1(15-45μM,48h)promotesapoptosisandblocksthecellcycleattheG0/G1phaseinprostatecancercellsincluding22RV1,PC-3,andLNCaPcells[1].SJL2-1(15-45μM)inhibitsPRMT5expression,reducesdownstreamSDMAlevelsandSmD3me2Sproteinexpression,anddecreasestheandrogenreceptorexpressionin22RV1,PC-3,andLNCaPcells[1].CellViabilityAssay[1]CellLine:PC3,22RV1,andLNCaPcellsConcentration:1-60μMIncubationTime:24,48,72,96hResult:Showedtheanti-proliferationinPC-3cellswithIC50sof46.11μM(24h),37.29μM(48h),32.74μM(72h)and26.24μM(96h).Showedtheanti-proliferationin22RV1cellswithIC50sof44.31μM(24h),40.07μM(48h),33.41μM(72h)and26.09μM(96h).Showedtheanti-proliferationinLNCAPcellswithIC50sof5.92μM(24h),4.29μM(481/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEh),4.68μM(72h)and4.45μM(96h).Immunofluorescence[1]CellLine:PC3,22RV1,andLNCaPcellsConcentration:23.055μM(PC3cells),22.155μM(22RV1cells),2.96μM(LNCAPcells)IncubationTime:24hResult:InhibitedcellproliferationandreducedactiveDNAreplicationin5-Ethynyl-2’-Deoxyuridine(EdU)(HY-118411)incorporationassay.CellMigrationAssay[1]CellLine:PC3,22RV1,andLNCaPcellsConcentration:23.055μM(PC3cells),22.155μM(22RV1cells),2.96μM(LNCAPcells)IncubationTime:48hResult:ReducedthenumberofmigratorycellsinPC-3,22RV1,andLNCaPcells.CellInvasionAssay[1]CellLine:PC3,22RV1,andLNCaPcellsConcentration:23.055μM(PC3cells),22.155μM(22RV1cells),2.96μM(LNCAPcells)IncubationTime:48hResult:SuppressedcellinvasionabilityinPC3,22RV1,andLNCaPcells.CellCycleAnalysis[1]CellLine:PC-3,22RV1,andLNCaPcellsConcentration:15,30,45μMIncubationTime:48hResult:Impededtheprogressionof22RV1,PC3,andLNCAPcellstotheG1phaseinadose-dependentmanner,withasignificantaccumulationofcellsintheG0/G1phaseandaconcomitantdecreaseinthenumberofcellsintheG2phase.WesternBlotAnalysis[1]CellLine:PC3,22RV1,andLNCaPcells2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEConcentration:15,30,45μMIncubationTime:48hResult:Upregulatedthepro-apoptoticeffectorBaxandelevatedlevelsofbothcaspase-3concentration-dependently.REFERENCES[1].DiaoT,etal.IdentificationofaSelectiveCell-ActiveInhibitorofProteinArginineMethyltransferase5(PRMT5)fortheTreatmentofProstateCancerbyStructure-BasedVirtualScreening.ChemBiolDrugDes.2025Jun;105(6):e70136.McePdfHeightCaution:Producthasnotbeenfull