SJL2-1-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESJL2-1Cat.No.:HY-174908分⼦式:C₂₂H₂₆N₂O分⼦量:334.45作⽤靶点:HistoneMethyltransferase;11β-HSD;AndrogenReceptor作⽤通路:Epigenetics;MetabolicEnzyme/Protease;VitaminDRelated/NuclearReceptor储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性SJL2-1⼀种PRMT5抑制剂，其IC50值为1.56μM。SJL2-1能抑制前列腺癌细胞的增殖、迁移和侵袭能⼒，促进细胞凋亡(apotosis)并使细胞周期阻滞于G0/G1期。SJL2-1可靶向细胞内的PRMT5结合，抑制雄激素受体的甲化及其表达。SJL2-1可⽤于早期雄激素敏感性前列腺癌和晚期去势抵抗性前列腺癌(CRPC)的相关研究[1]。体外研究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—您⾝边的抑制剂⼤师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—您⾝边的抑制剂⼤师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