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JQEZ-5

CAS No. 1913252-04-6

JQEZ-5 ( EZ-005 | EZ005 | JQEZ5 )

产品货号. M12997 CAS No. 1913252-04-6

一种新型有效、选择性、SAM 竞争性 EZH2 抑制剂,IC50 为 80 nM(抑制 PRC2 的酶功能)。

纯度: >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
5MG ¥721 有现货
10MG ¥1037 有现货
25MG ¥2122 有现货
50MG ¥3969 有现货
100MG ¥5792 有现货
200MG 获取报价 有现货
500MG 获取报价 有现货
1G 获取报价 有现货

生物学信息

  • 产品名称
    JQEZ-5
  • 注意事项
    本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
  • 产品简述
    一种新型有效、选择性、SAM 竞争性 EZH2 抑制剂,IC50 为 80 nM(抑制 PRC2 的酶功能)。
  • 产品描述
    A novel potent, selective, SAM-competitive EZH2 inhibitor with IC50 of 80 nM (inhibition of enzymatic function of PRC2); demonstrates acutely reduced level of H3K27me3 without affecting mono- and di-methylation, suppresses the proliferation of EZH2-overexpression H661 and H522 cell lines, more effectively than GSK-126 and GSK-343; promotes the regression of EZH2-driven tumors in vivo.
  • 体外实验
    JQEZ5 inhibits enzymatic functionality of PRC2 with a biochemical IC50 of 80nM. JQEZ5 exhibits S-adenosyl methionine (SAM)-competitive inhibition of PRC2.H661 cells treated with increasing concentrations of JQEZ5 demonstrate acutely reduced levels of H3K27me3 without affecting H3K27 mono- or di-methylation. JQEZ5 suppresses the proliferation of EZH2-overexpressing H661 and H522 cells after treatment for 4 days without affecting the proliferation of cell lines that were deemed insensitive to EZH2 knockdown.
  • 体内实验
    JQEZ5 (75 mg/kg; intraperitoneal injection; daily; for 3 weeks) treatment exhibits rapid and pronounced tumor regression over the three week treatment course. And H3K27me3 levels are largely reduced with treatment further confirming the on-target effect of JQEZ5 in mice.
  • 同义词
    EZ-005 | EZ005 | JQEZ5
  • 通路
    Chromatin/Epigenetic
  • 靶点
    HMTase
  • 受体
    HMTase
  • 研究领域
    ——
  • 适应症
    ——

化学信息

  • CAS Number
    1913252-04-6
  • 分子量
    542.688
  • 分子式
    C30H38N8O2
  • 纯度
    >98% (HPLC)
  • 溶解度
    DMSO : 25 mg/mL 46.07 mM;H2O : < 0.1 mg/mL
  • SMILES
    CC(C)N1N=CC2=C(C=C(N=C12)C3=CC=C(N4CCN(CC4)C)N=C3)C(NCC5=C(CCC)C=C(C)NC5=O)=O
  • 化学全称
    N-[(6-methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-6-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]-1-propan-2-ylpyrazolo[3,4-b]pyridine-4-carboxamide

运输与储存

  • 储存条件
    (-20℃)
  • 运输条件
    With Ice Pack
  • 稳定性
    ≥ 2 years

参考文献

1. Zhang H, et al. Cancer Discov. 2016 Sep;6(9):1006-21. 2. Frankel AE, et al. Cancer Discov. 2016 Sep;6(9):949-52.
产品手册
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