2. Epigenetics Apoptosis
  3. Histone Methyltransferase Apoptosis
  4. MM-401 TFA

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.

For research use only. We do not sell to patients.

MM-401 TFA Chemical Structure

MM-401 TFA Chemical Structure

CAS No. : 1442106-11-7

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of MM-401 TFA:

MM-401 TFA Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE MM-401 TFA

View All Histone Methyltransferase Isoform Specific Products:

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

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

IC50 & Target

Ki: < 1 nM (WDR5); IC50: 0.9 nM (WDR5-MLL1 interaction), 0.32 µM (MLL1)[1].
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.

MM-401 TFA Related Antibodies

Apoptosis Analysis[1]

Cell Line: Murine MLL-AF9 and Hoxa9/Meis1 cells
Concentration: 10, 20, 40 μM
Incubation Time: 48 h
Result: Specifically induced apoptosis of MLL-AF9 cells.

Cell Cycle Analysis[1]

Cell Line: Murine MLL-AF9 and Hoxa9/Meis1 cells
Concentration: 10, 20, 40 μM
Incubation Time: 48 h
Result: Induced prominent G1/S arrest in MLL-AF9 cells in a concentration dependent manner.

RT-PCR[1]

Cell Line: MLL-AF9 cells
Concentration: 20 μM
Incubation Time: 48 h
Result: Significantly decreased H3K4me, expression of 5 Hox A genes, especially Hoxa9 and Hoxa10.
Molecular Weight

700.75

Formula

C31H47F3N8O7
CAS No.
Appearance

Solid

Color

White to light yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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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.

  • Protocol 1

    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.
  • Protocol 2

    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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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.62%

COA (254 KB) RP-HPLC (244 KB) LCMS (259 KB)

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
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MM-401 TFA Related Classifications

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:

MM-4011442106-11-7MM401MM 401Histone MethyltransferaseApoptosisMLL1-WDR5 interactionMLL1histone methyltransferasesleukemiaH3K4cell cycleapoptosisdifferentiationInhibitorinhibitorinhibit

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