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 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.

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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 Related Antibodies

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EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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Description

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].

In Vitro

AF9/ENL-DOT1L/AF4 PPI-IN-1 (0-1μM, 3 days) significantly decreases the mRNA levels of Myc and Meis1 in a generally concentration-dependent manner in Molm-13 cells[1].
AF9/ENL-DOT1L/AF4 PPI-IN-1 can effectively and selectively inhibit a panel of cancer cells, including 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), and shows negligible antiproliferative activities against solid tumor HeLa cells(EC50 ＞ 30 μM)[1].

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

AF9/ENL-DOT1L PPI-IN-1 Related Antibodies

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.
In Vivo

AF9/ENL-DOT1L/AF4 PPI-IN-1 (25 mg/kg, 50 mg/kg, i.p., twice daily, 14 days) exhibits potent antitumor activity in an MLL-r leukemia NOD-SCID mice model, and the dose and regimen are well tolerated[1].
AF9/ENL-DOT1L/AF4 PPI-IN-1 (50 mg/kg, i.p., 0.5-24 h) has a favorable PK with a satisfactory plasma drug exposure and a long half-life of > 40 h in NOD-SCID mice[1].

MedChemExpress (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.
Molecular Weight

480.96

Formula

C26H26ClFN4O2
SMILES

FC1=CC=C(OC2=CC=C(NC3=CC=C4N=CC(OCC5CCNCC5)=NC4=C3)C=C2)C=C1.Cl
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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AF9/ENL-DOT1L PPI-IN-1 Related Classifications

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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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