Size | Price | Stock | Qty |
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1mg |
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5mg |
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Other Sizes |
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Targets |
Ki: < 1 nM (WDR5); IC50: 0.9 nM (WDR5-MLL1 interaction), 0.32 μM (MLL1)[1].
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ln Vitro |
MM-401 inhibits the WDR5-MLL1 interaction with an IC50 value of 0.9 nM while maintaining a strong binding affinity to WDR5 with a Ki value of < 1 nM[1]. By preventing the MLL1-WDR5 interaction and consequently the complex assembly, MM-401 can specifically inhibit MLL1 activity (IC50 value of 0.32µM)[1]. MLL1-dependent H3K4 methylation in cells is particularly inhibited by MM-401 (20 μM; 48 h)[1]. Similar alterations to the MLL-AF9 transcriptome are induced by MM-401 as by the MLL1 deletion[1]. MM-401 (10, 20, 40 μM; 48 h) specifically prevents MLL leukemia cells from growing by causing apoptosis and cell cycle arrest[1].
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Cell Assay |
Apoptosis Analysis[1]
Cell Types: Murine MLL-AF9 and Hoxa9/Meis1 cells Tested Concentrations: 10, 20, 40 μM Incubation Duration: 48 h Experimental Results: Specifically induced apoptosis of MLL-AF9 cells. Cell Cycle Analysis[1] Cell Types: Murine MLL-AF9 and Hoxa9/Meis1 cells Tested Concentrations: 10, 20, 40 μM Incubation Duration: 48 h Experimental Results: Induced prominent G1/S arrest in MLL-AF9 cells in a concentration dependent manner. RT-PCR[1] Cell Types: MLL-AF9 cells Tested Concentrations: 20 μM Incubation Duration: 48 h Experimental Results: Dramatically diminished H3K4me, expression of 5 Hox A genes, especially Hoxa9 and Hoxa10. |
References |
[1]. Fang Cao, et al. Targeting MLL1 H3K4 methyltransferase activity in mixed-lineage leukemia. Mol Cell. 2014 Jan 23;53(2):247-61.
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Molecular Formula |
C31H47F3N8O7
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Molecular Weight |
700.75
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CAS # |
1442106-11-7
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Related CAS # |
MM-401;1442106-10-6
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
C(F)(F)(F)C(=O)O.O=C1NCCCC[C@@](C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC)C(=O)N[C@]1([H])C1C=CC=CC=1)(C)NC(=O)C(C)C
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : 100 mg/mL (142.70 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.57 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.57 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (3.57 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.4270 mL | 7.1352 mL | 14.2704 mL | |
5 mM | 0.2854 mL | 1.4270 mL | 2.8541 mL | |
10 mM | 0.1427 mL | 0.7135 mL | 1.4270 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.