2. Epigenetics
  3. Histone Methyltransferase
  4. EPZ-4777

EPZ-4777 是一种选择性 DOT1L 抑制剂，可抑制癌细胞中 H3K79 甲基化，阻断致白血病基因的表达，并选择性杀死含有该基因易位的细胞。EPZ-4777 可用于肿瘤研究。

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EPZ-4777 Chemical Structure

EPZ-4777 Chemical Structure

CAS No. : 1381761-52-9

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EPZ-4777 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 NSD2/MMSET/WHSC1 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

EPZ-4777 is a selective DOT1L inhibitor which inhibits H3K79 methylation in cancer cells, blocks the expression of leukemogenic genes, and selectively kills cells that contain the translocation. EPZ-4777 can be used for cancer research[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
MV4-11 IC50
0.2 μM
Compound: 4
Induction of histone methylation in human MV4-11 cells assessed as H3K79 methylation after 4 days by Western blot analysis
Induction of histone methylation in human MV4-11 cells assessed as H3K79 methylation after 4 days by Western blot analysis
[PMID: 23795283]
MV4-11 EC50
4.4 μM
Compound: 55
Cytotoxicity against human MV4-11 cells harboring MLL-AF4 oncogene after 20 days by XTT assay
Cytotoxicity against human MV4-11 cells harboring MLL-AF4 oncogene after 20 days by XTT assay
[PMID: 22924785]
NB-4 EC50
101 μM
Compound: 55
Cytotoxicity against human NB4 cells harboring wild type MLL oncogene after 20 days by XTT assay
Cytotoxicity against human NB4 cells harboring wild type MLL oncogene after 20 days by XTT assay
[PMID: 22924785]
THP-1 EC50
8.1 μM
Compound: 55
Cytotoxicity against human THP1 cells harboring MLL-AF9 oncogene after 20 days by XTT assay
Cytotoxicity against human THP1 cells harboring MLL-AF9 oncogene after 20 days by XTT assay
[PMID: 22924785]
体外研究
(In Vitro)

EPZ-4777 (1-10000 nM, 24, 72 h) 剂量与时间依赖性地抑制 MOLM-13 细胞 HOXA9 和 LSD1 的表达[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

EPZ-4777 相关抗体:
分子量

540.66

Formula

C27H40N8O4
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

EPZ-4777 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • 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:

EPZ-47771381761-52-9EPZ4777EPZ 4777Histone MethyltransferaseDOT1LH3K79 methylationleukemogenic genecancerInhibitorinhibitorinhibit

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产品名称：
EPZ-4777
目录号：
HY-111589
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