1. Epigenetics
  2. Histone Methyltransferase
  3. EZH2-IN-1

EZH2-IN-1 (compound 3) 是一种选择性且 SAM 竞争性的 EZH2EZH1 抑制剂,对 EZH2wt、EZH2 Y641N 突变体和 EZH1IC50 值分别为 32 nM、197 nM 和 213 nM。EZH2-IN-1 降低了 H3K27me3 和 H3K27me2 的总体水平。EZH2-IN-1具有用于弥漫性大B细胞淋巴瘤研究的潜力。

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EZH2-IN-1

EZH2-IN-1 Chemical Structure

CAS No. : 1377997-28-8

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EZH2-IN-1 (compound 3) is a selective and SAM-competitive EZH2 and EZH1 inhibitor with an IC50s of 32 nM, 197 nM and 213 nM for EZH2wt, EZH2 Y641N mutant and EZH1, respectively. EZH2-IN-1 reduces bulk H3K27me3 and H3K27me2 levels. EZH2-IN-1 has the potential for diffuse large B cell lymphoma research[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HeLa EC50
7 μM
Compound: 23
Inhibition of EZH2 in human HeLa cells assessed as reduction of H3K27me3 and H3K27me2 level after 96 hrs by ELISA method
Inhibition of EZH2 in human HeLa cells assessed as reduction of H3K27me3 and H3K27me2 level after 96 hrs by ELISA method
[PMID: 25406853]
KARPAS-422 GI50
13.2 μM
Compound: 44
Growth inhibition of human KARPAS422 cells after 14 days by Cell-Titer luminescence assay
Growth inhibition of human KARPAS422 cells after 14 days by Cell-Titer luminescence assay
[PMID: 24900844]
KARPAS-422 GI50
23 μM
Compound: 44
Growth inhibition of human KARPAS422 cells after 10 days by Cell-Titer luminescence assay
Growth inhibition of human KARPAS422 cells after 10 days by Cell-Titer luminescence assay
[PMID: 24900844]
KARPAS-422 GI50
24.8 μM
Compound: 44
Growth inhibition of human KARPAS422 cells after 7 days by Cell-Titer luminescence assay
Growth inhibition of human KARPAS422 cells after 7 days by Cell-Titer luminescence assay
[PMID: 24900844]
KARPAS-422 GI50
70 μM
Compound: 44
Growth inhibition of human KARPAS422 cells after 4 days by Cell-Titer luminescence assay
Growth inhibition of human KARPAS422 cells after 4 days by Cell-Titer luminescence assay
[PMID: 24900844]
KARPAS-422 GI50
9.1 μM
Compound: 44
Growth inhibition of human KARPAS422 cells after 17 days by Cell-Titer luminescence assay
Growth inhibition of human KARPAS422 cells after 17 days by Cell-Titer luminescence assay
[PMID: 24900844]
分子量

490.00

Formula

C27H28ClN5O2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
EZH2-IN-1
目录号:
HY-122595
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