2. Epigenetics
  3. Histone Methyltransferase
  4. Dot1L-IN-1

Dot1L-IN-1 是一种高效的选择性 Dot1L 抑制剂，Ki 为 2 pM，IC50<0.1 nM。Dot1L-IN-1 有效抑制 HeLa 细胞中 H3K79 二甲基化 (IC50=3 nM) 以及 Molm-13 细胞中 HoxA9 启动子的活性 (IC50=17 nM)。

在相同的摩尔浓度下，化合物盐形式与游离形式有相同的生物活性，但盐形式 Dot1L-IN-1 TFA 通常具有更好的水溶性和稳定性。

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Dot1L-IN-1 Chemical Structure

Dot1L-IN-1 Chemical Structure

CAS No. : 2088518-50-5

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Dot1L-IN-1 的其他形式现货产品:

Customer Review

Other Forms of Dot1L-IN-1:

Dot1L-IN-1 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

Dot1L-IN-1 is a highly potent and selective Dot1L inhibitor with a Ki of 2 pM and an IC50 of <0.1 nM. Dot1L-IN-1 potently suppresses H3K79 dimethylation (IC50=3 nM), as well as the activity of the HoxA9 promoter (IC50=17 nM) in HeLa and Molm-13 cells, respectively[1].

IC50 & Target[1]

DOT1L

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HeLa IC50
3 nM
Compound: 7
Inhibition of DOT1L in human HeLa cells assessed as reduction in H3K79me2 level after 72 hrs by ELISA
Inhibition of DOT1L in human HeLa cells assessed as reduction in H3K79me2 level after 72 hrs by ELISA
[PMID: 28337327]
MV4-11 IC50
5 nM
Compound: 7
Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 treated for 6 hrs measured after 8 days by Celltiter-Glo reagent based assay
Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 treated for 6 hrs measured after 8 days by Celltiter-Glo reagent based assay
[PMID: 28337327]
体外研究
(In Vitro)

Dot1L-IN-1 (类似物 7) 有效抑制携带致癌 MLL-AF4 融合的人 MLL 重排白血病细胞系 MV4-11 的增殖 (IC50=5 nM)[1 ]。

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

Dot1L-IN-1 相关抗体:
分子量

646.21

Formula

C32H36ClN9O2S
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

Dot1L-IN-1 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:

Dot1L-IN-12088518-50-5Histone MethyltransferaseDot1LH3K79 dimethylationHoxA9 promoterHeLaMolm-13Inhibitorinhibitorinhibit

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