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Purity: ≥98%
MM-401 is a novel, potent and selective inhibitor of histone H3K4 methyltransferase MLL1 activity. MM-401 acts by reprograming mouse epiblast stem cells (EpiSCs) to naive pluripotency.
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 complex assembly and MLL1-WDR5 interaction, MM-401 can specifically reduce MLL1 activity (IC50 value: 0.32μM) [1]. Specifically, MLL1-dependent H3K4 methylation in cells is inhibited by MM-401 (20 μM; 48 hours) [1]. Similar alterations to the MLL-AF9 transcriptome are caused by MM-401 and MLL1 deletion [1]. By causing cell cycle arrest and death, MM-401 (10, 20, 40 μM; 48 h) specifically suppresses the development of MLL leukemia cells [1].
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Cell Assay |
Apoptosis analysis [1]
Cell Types: mouse MLL-AF9 and Hoxa9/Meis1 cells Tested Concentrations: 0, 20, 40 μM Incubation Duration: 48 h Experimental Results: Specific induction of MLL-AF9 cell apoptosis. Cell cycle analysis [1] Cell Types: mouse MLL-AF9 and Hoxa9/Meis1 Cell Tested Concentrations: 10, 20, 40 μM Incubation Duration: 48 hrs (hours) Experimental Results: Significant G1/ was induced in MLL-AF9 cells in a concentration-dependent manner S Stasis. RT-PCR[1] Cell Types: MLL-AF9 Cell Tested Concentrations: 20 μM Incubation Duration: 48 hrs (hours) Experimental Results: H3K4me, the expression of 5 Hox A genes was Dramatically diminished, 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 |
C29H46N8O5
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Molecular Weight |
586.73
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Exact Mass |
586.3591
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CAS # |
1442106-10-6
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Related CAS # |
MM-401 TFA;1442106-11-7
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SMILES |
CC(C)C(N[C@@]1(C)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC)C(N[C@H](C2=CC=CC=C2)C(NCCCC1)=O)=O)=O)=O)=O
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Chemical Name |
N-[6(S)-Ethyl-9(S)-(3-guanidino-propyl)-12(R)-methyl-2,5,8,11-tetraoxo-3(R)-phenyl-1,4,7,10tetraaza-cyclohexadec-12-yl]-isobutyramide
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Synonyms |
MM 401MM-401 MM401
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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 Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.7044 mL | 8.5218 mL | 17.0436 mL | |
5 mM | 0.3409 mL | 1.7044 mL | 3.4087 mL | |
10 mM | 0.1704 mL | 0.8522 mL | 1.7044 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.