EZH2-IN-14

• 常用名: EZH2-IN-14
• 英文名: EZH2-IN-14
• CAS号: 1979157-17-9
• 分子量: 541.69
• 密度: N/A
• 沸点: N/A
• 分子式: C₃₁H₃₉N₇O₂
• 熔点: N/A
• 闪点: N/A

EZH2-IN-14用途

EZH2-IN-14是一种选择性的EZH2(组蛋白甲基转移酶)抑制剂,IC50为12nM。EZH2-IN-14抑制EZH2/PRC2的甲基转移酶活性(即减少H3K27me3)。EZH2-IN-14对EZH2的选择性是高度同源的H3K27甲基转移酶EZH1[1]的200倍以上。

EZH2-IN-14名称

• 英文名: EZH2-IN-14

EZH2-IN-14生物活性

• 描述: EZH2-IN-14是一种选择性的EZH2(组蛋白甲基转移酶)抑制剂,IC50为12nM。EZH2-IN-14抑制EZH2/PRC2的甲基转移酶活性(即减少H3K27me3)。EZH2-IN-14对EZH2的选择性是高度同源的H3K27甲基转移酶EZH1[1]的200倍以上。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 表观遗传学 >> 组蛋白甲基转移酶
• 体外研究: EZH2-IN-14(C24)有效减少H3K27立方米和 H3K27平方米蛋白水平,但对 MDA-MB-468型细胞中 EZH2型蛋白水平影响不大[1]。 细胞活力测定[1]细胞系：MDA-MB-468细胞浓度：4μM培养时间：6小时、12小时、24小时、48小时结果：H3K27me3和H3K27me2标记降低。
• 参考文献:

  [1]. Anqi Ma, et al. Discovery of a first-in-class EZH2 selective degrader. Nat Chem Biol. 2020 Feb;16(2):214-222.

EZH2-IN-14物理化学性质

• 分子式: C₃₁H₃₉N₇O₂
• 分子量: 541.69

EZH2-IN-14靶点实验

查看更多实验

实验名称：Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay 来源：ChEMBL 靶标：A549 External Id：CHEMBL5327794

实验名称：Binding affinity to recombinant PRC2 complex (unknown origin) assessed as dissociatio... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5111868

实验名称：Binding affinity to recombinant PRC2 complex (unknown origin) assessed as association... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5111869

实验名称：Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by MTT... 来源：ChEMBL 靶标：MDA-MB-231 External Id：CHEMBL5327792

实验名称：Antiproliferative activity against human BT-549 cells incubated for 72 hrs by MTT ass... 来源：ChEMBL 靶标：BT-549 External Id：CHEMBL5327793

实验名称：Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by MTT as... 来源：ChEMBL 靶标：HCT-116 External Id：CHEMBL5327791

实验名称：Inhibition of EZH2 histone methyltransferase activity of EZH2/EED/SUZ12 protein compl... 来源：ChEMBL 靶标：Histone-lysine N-methyltransferase EZH2 External Id：CHEMBL4479462

实验名称：Synergistic antiproliferative activity against human MV4-11 cells assessed as combina... 来源：ChEMBL 靶标：MV4-11 External Id：CHEMBL5111918

实验名称：Inhibition of EZH1 histone methyltransferase activity of EZH1/EED/SUZ12/RBBP4/AEBP2 p... 来源：ChEMBL 靶标：Histone-lysine N-methyltransferase EZH1 External Id：CHEMBL4479463

实验名称：Synergistic antiproliferative activity against human SU-DHL-10 cells assessed as comb... 来源：ChEMBL 靶标：SU-DHL10 External Id：CHEMBL5111919

共19条，当前第1页，共2页

1

2