1. Epigenetics
  2. Epigenetic Reader Domain
  3. MI-2-2

MI-2-2 is a potent menin-MLL inhibitor. MI-2-2 binds to menin with low nanomolar affinity (Kd=22nM) and very effectively disrupts the bivalent protein-protein interaction between menin and MLL. MI-2-2 has specific and very pronounced activity in MLL leukemia cells, including inhibition of cell proliferation, down-regulation of Hoxa9 expression, and differentiation.

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

MI-2-2 Chemical Structure

MI-2-2 Chemical Structure

CAS No. : 1454920-20-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 319 In-stock
Solution
10 mM * 1 mL in DMSO USD 319 In-stock
Solid
5 mg USD 290 In-stock
10 mg USD 420 In-stock
25 mg USD 780 In-stock
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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

MI-2-2 is a potent menin-MLL inhibitor. MI-2-2 binds to menin with low nanomolar affinity (Kd=22nM) and very effectively disrupts the bivalent protein-protein interaction between menin and MLL. MI-2-2 has specific and very pronounced activity in MLL leukemia cells, including inhibition of cell proliferation, down-regulation of Hoxa9 expression, and differentiation[1].

Cellular Effect
Cell Line Type Value Description References
K562 IC50
> 20 μM
Compound: 1; MI-2-2
Antiproliferative activity against human K562 cells after 7 days by MTS assay
Antiproliferative activity against human K562 cells after 7 days by MTS assay
[PMID: 27528435]
MV4-11 IC50
0.64 μM
Compound: 1; MI-2-2
Antiproliferative activity against human MV4-11 cells expressing MLL-AF4 after 7 days by MTS assay
Antiproliferative activity against human MV4-11 cells expressing MLL-AF4 after 7 days by MTS assay
[PMID: 27528435]
MV4-11 IC50
2.6 μM
Compound: MI-2-2
Antiproliferative activity against human MV4-11 cells after 168 hrs by MTS assay
Antiproliferative activity against human MV4-11 cells after 168 hrs by MTS assay
[PMID: 30713023]
In Vitro

MI-2-2 is capable of inhibiting both the interaction of menin with MBM1 (IC50= 46 nM) and with the bivalent fragment of MLL that comprises both MBM1 and MBM2 (IC50=520 nM). MI-2-2 exhibits very pronounced activities at low micromolar concentrations in BMCs transformed with MLL-AF9 and in MV4;11, a human leukemia cell line harboring the MLL-AF4 translocation[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

415.50

Formula

C17H20F3N5S2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC(F)(F)CC1=CC2=C(N3CCN(C4=NCC(C)(C)S4)CC3)N=CN=C2S1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (240.67 mM; Need ultrasonic; 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 2.4067 mL 12.0337 mL 24.0674 mL
5 mM 0.4813 mL 2.4067 mL 4.8135 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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C2

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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    90% Corn Oil

    Solubility: ≥ 3.75 mg/mL (9.03 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
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 (sealed storage, away from moisture and 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: 99.92%

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 (sealed storage, away from moisture and 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 2.4067 mL 12.0337 mL 24.0674 mL 60.1685 mL
5 mM 0.4813 mL 2.4067 mL 4.8135 mL 12.0337 mL
10 mM 0.2407 mL 1.2034 mL 2.4067 mL 6.0168 mL
15 mM 0.1604 mL 0.8022 mL 1.6045 mL 4.0112 mL
20 mM 0.1203 mL 0.6017 mL 1.2034 mL 3.0084 mL
25 mM 0.0963 mL 0.4813 mL 0.9627 mL 2.4067 mL
30 mM 0.0802 mL 0.4011 mL 0.8022 mL 2.0056 mL
40 mM 0.0602 mL 0.3008 mL 0.6017 mL 1.5042 mL
50 mM 0.0481 mL 0.2407 mL 0.4813 mL 1.2034 mL
60 mM 0.0401 mL 0.2006 mL 0.4011 mL 1.0028 mL
80 mM 0.0301 mL 0.1504 mL 0.3008 mL 0.7521 mL
100 mM 0.0241 mL 0.1203 mL 0.2407 mL 0.6017 mL
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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.

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Product Name:
MI-2-2
Cat. No.:
HY-108350
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