MM-401 TFA
Based on 1 publication(s) in Google Scholar
MM-401 (TFA) is a MLL1 H3K4 methyltransferase inhibitor. MM-401 inhibits MLL1 activity (IC50 = 0.32 μM) by blocking MLL1-WDR5 interaction. MM-401 can induce cell cycle arrest, apoptosis and differentiation. MM-401 can be used for the research of MLL leukemia.
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- Purity: 99.34%
- CAS No.: 1442106-11-7
- 화학식: C31H47F3N8O7
- 분자량:700.75
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보관:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) MM-401 TFA
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Biological Activity
제품 설명
IC50 & Target
Ki: < 1 nM (WDR5); IC50: 0.9 nM (WDR5-MLL1 interaction), 0.32 µM (MLL1)[1].
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HL-60 | IC50 |
>100 μM
Compound: 2
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Cytotoxicity against human HL60 cells lacking MLL translocation assessed as cell growth inhibition after 4 days by WST8 assay
Cytotoxicity against human HL60 cells lacking MLL translocation assessed as cell growth inhibition after 4 days by WST8 assay
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[PMID: 28603984] |
| MOLM-13 | IC50 |
18.4 μM
Compound: 2
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Cytotoxicity against human MOLM13 cells harboring MLL-AF9 fusion protein assessed as cell growth inhibition after 4 days by WST8 assay
Cytotoxicity against human MOLM13 cells harboring MLL-AF9 fusion protein assessed as cell growth inhibition after 4 days by WST8 assay
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[PMID: 28603984] |
| MV4-11 | IC50 |
9.8 μM
Compound: 2
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Cytotoxicity against human MV4-11 cells harboring MLL-AF4 fusion protein assessed as cell growth inhibition after 4 days by WST8 assay
Cytotoxicity against human MV4-11 cells harboring MLL-AF4 fusion protein assessed as cell growth inhibition after 4 days by WST8 assay
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[PMID: 28603984] |
In Vitro
MM-401 maintains high binding affinity to WDR5 with a Ki value of < 1 nM and disrupts WDR5-MLL1 interaction with an IC50 value of 0.9 nM[1].
MM-401 is able to specifically inhibit MLL1 activity (IC50 value of 0.32μM) by blocking MLL1-WDR5 interaction and thus the complex assembly[1].
MM-401 (20 μM; 48 h) specifically inhibits MLL1-dependent H3K4 methylation in cells[1].
MM-401 induces similar changes in MLL-AF9 transcriptome as the MLL1 deletion[1].
MM-401 (10, 20, 40 μM; 48 h) specifically inhibits growth of MLL leukemia cells by inducing cell cycle arrest, apoptosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Murine MLL-AF9 and Hoxa9/Meis1 cells
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Concentration:10, 20, 40 μM
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Incubation Time:48 h
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Result:Specifically induced apoptosis of MLL-AF9 cells.
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Cell Line:Murine MLL-AF9 and Hoxa9/Meis1 cells
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Concentration:10, 20, 40 μM
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Incubation Time:48 h
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Result:Induced prominent G1/S arrest in MLL-AF9 cells in a concentration dependent manner.
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Cell Line:MLL-AF9 cells
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Concentration:20 μM
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Incubation Time:48 h
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Result:Significantly decreased H3K4me, expression of 5 Hox A genes, especially Hoxa9 and Hoxa10.
Chemical Information
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CAS No. 1442106-11-7
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Appearance Solid
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분자량 700.75
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화학식 C31H47F3N8O7
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Color White to light yellow
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SMILES
C[C@@](C(N[C@@H](CCCNC(N)=N)C(N[C@H](C(N[C@@]1(C2=CC=CC=C2)[H])=O)CC)=O)=O)(NC(C(C)C)=O)CCCCNC1=O.O=C(O)C(F)(F)F
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
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Nat Commun
KMT2A associates with PHF5A-PHF14-HMG20A-RAI1 subcomplex in pancreatic cancer stem cells and epigenetically regulates their characteristics. [Abstract]2023 Sep 14;14(1):5685. PMID: 37709746
용액&용해도
In Vitro:
DMSO : 100 mg/mL (142.70 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.57 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.57 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.4270 mL | 7.1352 mL | 14.2704 mL | 35.6761 mL |
| 5 mM | 0.2854 mL | 1.4270 mL | 2.8541 mL | 7.1352 mL | |
| 10 mM | 0.1427 mL | 0.7135 mL | 1.4270 mL | 3.5676 mL | |
| 15 mM | 0.0951 mL | 0.4757 mL | 0.9514 mL | 2.3784 mL | |
| 20 mM | 0.0714 mL | 0.3568 mL | 0.7135 mL | 1.7838 mL | |
| 25 mM | 0.0571 mL | 0.2854 mL | 0.5708 mL | 1.4270 mL | |
| 30 mM | 0.0476 mL | 0.2378 mL | 0.4757 mL | 1.1892 mL | |
| 40 mM | 0.0357 mL | 0.1784 mL | 0.3568 mL | 0.8919 mL | |
| 50 mM | 0.0285 mL | 0.1427 mL | 0.2854 mL | 0.7135 mL | |
| 60 mM | 0.0238 mL | 0.1189 mL | 0.2378 mL | 0.5946 mL | |
| 80 mM | 0.0178 mL | 0.0892 mL | 0.1784 mL | 0.4460 mL | |
| 100 mM | 0.0143 mL | 0.0714 mL | 0.1427 mL | 0.3568 mL |
MM-401 TFA Related Classifications
HY-19554A Related Classifications
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