2. Epigenetics Apoptosis Cell Cycle/DNA Damage
  3. Histone Methyltransferase c-Myc Epigenetic Reader Domain HOXA
  4. AF9/ENL-DOT1L PPI-IN-1

AF9/ENL-DOT1L/AF4 PPI-IN-1 是 AF9/ENL 和组蛋白甲基转移酶 DOT1L/AF4 蛋白质-蛋白质相互作用 (PPI) 的强效抑制剂。AF9/ENL-DOT1L/AF4 PPI-IN-1 可抑制 AF9-DOT1L (IC50 = 1.5 μM)、AF9-AF4 (IC50 = 1 μM) 和 ENL-AF4 (IC50 = 1.2 μM) 相互作用。AF9/ENL-DOT1L/AF4 PPI-IN-1 可抑制混合谱系白血病 (MLL) 靶基因 Myc 和 Meis1 的表达，并选择性阻断 MLL-r 和其他几种白血病细胞的增殖。AF9/ENL-DOT1L/AF4 PPI-IN-1 在小鼠 MLL-r 白血病模型中表现出显著的抗肿瘤活性，且无明显毒性。 AF9/ENL-DOT1L/AF4 PPI-IN-1 可用于 MLL-r 白血病的研究。

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AF9/ENL-DOT1L PPI-IN-1

AF9/ENL-DOT1L PPI-IN-1 Chemical Structure

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AF9/ENL-DOT1L PPI-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 ASH1L/KMT2H 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

AF9/ENL-DOT1L/AF4 PPI-IN-1 is a potent AF9/ENL and histone methyltransferase DOT1L/AF4 protein-protein interactions (PPI) inhibitor. AF9/ENL-DOT1L/AF4 PPI-IN-1 can inhibit the AF9-DOT1L (IC50 = 1.5 μM), AF9-AF4 (IC50 = 1 μM), ENL-AF4 (IC50 = 1.2 μM) interactions. AF9/ENL-DOT1L/AF4 PPI-IN-1 can suppress the expression of Mixed lineage leukemia (MLL) target genes Myc and Meis1 and selectively block the proliferation of MLL-r and several other leukemia cells. AF9/ENL-DOT1L/AF4 PPI-IN-1 exhibits significant antitumor activities in a mouse model of MLL-r leukemia without overt toxicities. AF9/ENL-DOT1L/AF4 PPI-IN-1 can be used for the study of MLL-r leukemia[1].

体外研究
(In Vitro)

AF9/ENL-DOT1L/AF4 PPI-IN-1 (0-1 μM，3 天) 显著降低 Molm-13 细胞中 Myc 和 Meis1 的 mRNA 水平，且呈浓度依赖性[1]。
AF9/ENL-DOT1L/AF4 PPI-IN-1 可以有效且选择性地抑制一组癌细胞，包括 MV4-11 (EC50 = 0.96 μM)、Molm-13 (EC50 = 1.6 μM)、NB4 (EC50 = 2.7 μM)、HL-60 (EC50 = 0.66 μM)、Kasumi (EC50 = 0.92 μM)、Jurkat (EC50 = 0.77 μM)，并且对实体瘤 HeLa 细胞表现出可忽略不计的抗增殖活性 (EC50 ＞ 30 μM)[1]。

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

AF9/ENL-DOT1L PPI-IN-1 相关抗体:

RT-PCR[1]

Cell Line: Molm-13 cells
Concentration: 0 μM, 0.3 μM, 1μM
Incubation Time: 72 h
Result: Significantly decreased the mRNA levels of Myc and Meis1 in a generally concentration-dependent manner in Molm-13 cells.
体内研究
(In Vivo)

AF9/ENL-DOT1L/AF4 PPI-IN-1 (25 mg/kg，50 mg/kg，腹腔注射，每日两次，共 14 天) 在 MLL-r 白血病 NOD-SCID 小鼠模型中表现出强效的抗肿瘤活性，且该剂量和给药方案耐受性良好[1]。
AF9/ENL-DOT1L/AF4 PPI-IN-1 (50 mg/kg，腹腔注射，0.5-24 小时) 在 NOD-SCID 小鼠中具有良好的药代动力学特性，血浆药物暴露量令人满意，半衰期 > 40小时[1]。

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

Animal Model: 106 Molm-13 cells were injected subcutaneously into 6−8 weeks old NOD-SCID mice[1].
Dosage: 1-3 days, 50 mg/kg, twice daily
4-14 days, 25 mg/kg, twice daily
Administration: I.p.
Result: Significantly inhibited tumor growth in mice by 65%.
After 24 h, its plasma concentration was 1.7 μM, which is well above the EC50 values of AF9/ENL-DOT1L/AF4 PPI-IN-1 against the two MLL-r leukemia cells.
Animal Model: NOD-SCID mice.
Dosage: 50 mg/kg
Administration: I.p.
Result: Exhibited a favorable PK profile with the maximal plasma concentration of 3.1 μM and a half-life of > 40 h.
分子量

480.96

Formula

C26H26ClFN4O2
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

AF9/ENL-DOT1L PPI-IN-1 相关分类

  • 摩尔计算器

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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:

AF9/ENL-DOT1L PPI-IN-1Histone Methyltransferasec-MycEpigenetic Reader DomainHOXAMycHomeobox AMixed lineage leukemiaMLLProtein-protein interactionsPPIAF9/ENLDOT1LMeis1Inhibitorinhibitorinhibit

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