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DC-PRC2in-01

Cat.No.:HY-178694

CASNo.:120430-77-5

分⼦式:C₂₇H₂₉FN₄O

分⼦量:444.54

作⽤靶点:HistoneMethyltransferase

作⽤通路:Epigenetics

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性DC-PRC2in-01是⼀种强效的EZH2-EED相互作⽤抑制剂，其IC50为4.21μM，Kd为4.56μM。DC-PRC2in-

01破坏PRC2复合体的稳定性，导致PRC2核⼼蛋⽩降解和H3K27me3⽔平降低，从⽽抑制PRC2驱动的淋巴

瘤细胞增殖并导致细胞周期阻滞。DC-PRC2in-01可⽤于研究PRC2相关的癌症，如弥漫性⼤B细胞淋巴瘤(

DLBCL)和滤泡性淋巴瘤(FL)[1]。

IC50TargetEZH2

体外研究DC-PRC2in-01(3days)suppressesproliferationofDLBCLcelllines(Pfeiffer,SU-DHL-4,KARPAS-422,and

DBcells)withIC50valuesof3.77,5.97,5.87,and9.62μM,respectively.[1].

DC-PRC2in-01(0.625-5μM,2-3days)dose-dependentlyinducesG0/G1phasecellcyclearrestsinPfeiffer

andSU-DHL-4cells[1].

DC-PRC2in-01(0-10μM,3days)specificallyinhibitsthePRC2activitybydisruptingtheEZH2-EED

interaction,leadingtothedepletionofPRC2corecomponentsinPfeiffercells,resultinginadose-dependent

decreaseofH3K27me3levels[1].

CellCycleAnalysis[1]

CellLine: