2. Epigenetics
  3. Histone Methyltransferase
  4. IHMT-EZH2-426

IHMT-EZH2-426 (compound 38) 是一种有效的共价 EZH2 降解剂，针对 EZH2 野生型、EZH2-A687V 和 EZH2-Y641F/Y641N/Y641S 的 IC50 分别为 1.3 nM、1.2 nM 和 1.7-3.5 nM 。IHMT-EZH2-426 通过降低 H3K27me3 和 EZH2 的水平，对 B 细胞淋巴瘤和三阴性乳腺癌 (TNBC) 细胞系表现出有效的抗增殖作用。

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IHMT-EZH2-426 Chemical Structure

IHMT-EZH2-426 Chemical Structure

CAS No. : 3018914-66-1

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IHMT-EZH2-426 相关抗体

Top Publications Citing Use of Products

查看 Histone Methyltransferase 亚型特异性产品:

查看所有亚型
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

IHMT-EZH2-426 (compound 38) is a potent and covalent EZH2 degrader with IC50s of 1.3 nM, 1.2 nM, and 1.7-3.5 nM against EZH2 wild-type, EZH2-A687V, and EZH2-Y641F/Y641N/Y641S, respectively. IHMT-EZH2-426 exhibits potent antiproliferation effects against both B-cell lymphoma and triple negative breast cancer (TNBC) cell lines by reducing the levels of H3K27me3 and EZH2[1].

IC50 & Target[1]

EZH2 WT

1.3 nM (IC50)

EZH2-A687V

1.2 nM (IC50)

Y641F/Y641N/Y641S

1.7-3.5 nM (IC50)

分子量

578.70

Formula

C31H35FN4O4S
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

IHMT-EZH2-426 相关分类

  • 摩尔计算器

  • 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.

Keywords:

IHMT-EZH2-4263018914-66-1Histone MethyltransferaseY641FY641NY641Sand A687Vcovalent EZH2 degraderantiproliferation effectsH3K27me3Inhibitorinhibitorinhibit

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产品名称：
IHMT-EZH2-426
目录号：
HY-156292
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