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AF9/ENL-DOT1L PPI-IN-1
Catalog No. T213481 Copy Product Info
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AF9/ENL-DOT1L/AF4 PPI-IN-1 is a potent inhibitor of protein-protein interactions (PPI) between AF9/ENL and the histone methyltransferase DOT1L/AF4. It effectively inhibits the interactions of AF9-DOT1L (IC50= 1.5 μM), AF9-AF4 (IC50= 1 μM), and ENL-AF4 (IC50= 1.2 μM). This compound suppresses the expression of MLL target genes, Myc and Meis1, and selectively blocks the proliferation of MLL-r and other leukemia cells. In a mouse model of MLL-r leukemia, AF9/ENL-DOT1L/AF4 PPI-IN-1 demonstrates significant antitumor activity with no notable toxicity. It is a useful agent for studying MLL-r leukemia.
AF9/ENL-DOT1L PPI-IN-1
Copy Product Info🥰Excellent
Catalog No. T213481
AF9/ENL-DOT1L/AF4 PPI-IN-1 is a potent inhibitor of protein-protein interactions (PPI) between AF9/ENL and the histone methyltransferase DOT1L/AF4. It effectively inhibits the interactions of AF9-DOT1L (IC50= 1.5 μM), AF9-AF4 (IC50= 1 μM), and ENL-AF4 (IC50= 1.2 μM). This compound suppresses the expression of MLL target genes, Myc and Meis1, and selectively blocks the proliferation of MLL-r and other leukemia cells. In a mouse model of MLL-r leukemia, AF9/ENL-DOT1L/AF4 PPI-IN-1 demonstrates significant antitumor activity with no notable toxicity. It is a useful agent for studying MLL-r leukemia.
AF9/ENL-DOT1L PPI-IN-1
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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For research use only—not for human use. No sales to individuals. Use as intended only.
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| Description | AF9/ENL-DOT1L/AF4 PPI-IN-1 is a potent inhibitor of protein-protein interactions (PPI) between AF9/ENL and the histone methyltransferase DOT1L/AF4. It effectively inhibits the interactions of AF9-DOT1L (IC50= 1.5 μM), AF9-AF4 (IC50= 1 μM), and ENL-AF4 (IC50= 1.2 μM). This compound suppresses the expression of MLL target genes, Myc and Meis1, and selectively blocks the proliferation of MLL-r and other leukemia cells. In a mouse model of MLL-r leukemia, AF9/ENL-DOT1L/AF4 PPI-IN-1 demonstrates significant antitumor activity with no notable toxicity. It is a useful agent for studying MLL-r leukemia. |
| In vitro | AF9/ENL-DOT1L/AF4 PPI-IN-1 (0-1 μM，3 days) significantly reduces the mRNA levels of Myc and Meis1 in a concentration-dependent manner in Molm-13 cells. AF9/ENL-DOT1L/AF4 PPI-IN-1 effectively and selectively inhibits a range 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), and Jurkat (EC₅₀ = 0.77 μM), while showing negligible antiproliferative activity against solid tumor HeLa cells (EC₅₀ > 30 μM). |
| In vivo | AF9/ENL-DOT1L/AF4 PPI-IN-1, administered at 25 mg/kg and 50 mg/kg twice daily via intraperitoneal injection for 14 days, demonstrates significant antitumor activity in an MLL-r leukemia NOD-SCID mouse model, with good tolerance at these dosages. Additionally, at 50 mg/kg via intraperitoneal injection (0.5-24 hours), it exhibits favorable pharmacokinetic properties in NOD-SCID mice, with satisfactory plasma drug exposure and a half-life exceeding 40 hours. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
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