JCS-1-生命科学试剂-MCE-4278

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEJCS-1Cat.No.:HY-164977分⼦式:C₆₂H₇₉N₉O₁₂S分⼦量:1174.41作⽤靶点:PROTACs;Phosphatase作⽤通路:PROTAC;MetabolicEnzyme/Protease储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性JCS-1⼀种强效的DcpSPROTAC降解剂。JCS-1通过于RG3039的弹头与DcpS⾮共价结合，并招募E3连接酶VHL。JCS-1可在纳尔浓度下促进DcpS泛素化和降解(在MOLM-14细胞中的DC50为87nM)。JCS-1可⽤于急性髓细胞性⽩⾎病和其他依赖DcpS的遗传性疾病研究(粉红：DcpS配体(HY-102020)；蓝⾊：E3连接酶VHL配体(HY-151227)；⿊⾊：连接⼦(HY-141230))[1]。IC50&TargetVHL体外研究JCS-1(0.1-10000nM,24h)degradesDcpSinMOLM-14cellsinadose-dependentmannerwithaDC50of87nM[1].JCS-1(1μM)degradesDcpSrapidlyandcontinuouslyinMOLM-14cells,withdegradationoccurringrapidlywithin2hoftreatmentandmaximumdegradationoccurringbetween12and24h[1].JCS-1(1μM,every3daysfor12days)inhibitstheproliferationandviabilityofMOLM-14cellswithanIC50valueof1.1μM[1].JCS-1(1μM,6h)influencesthemRNApoolofMOLM-14cellswithsignificantincreaseinSNORD99andDDX24expression[1].DegradationbyJCS-1isinhibitedbytheneddylationinhibitorMLN4924(HY-70062)andproteasomeinhibitorEpoxomicin(HY-13821)[1].REFERENCES[1].Swartzel,etal.TargetedDegradationofmRNADecappingEnzymeDcpSbyaVHL-RecruitingPROTAC.ACSchemicalbiology.2022,17(7),1789–1798.McePdfHeight1/1MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792/p>