2. Epigenetics
  3. Epigenetic Reader Domain
  4. MI-538

MI-538 is an inhibitor of the interaction between menin and MLL fusion proteins with an IC50 of 21 nM.

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

MI-538 Chemical Structure

MI-538 Chemical Structure

CAS No. : 1857417-10-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 299 In-stock
Solution
10 mM * 1 mL in DMSO USD 299 In-stock
Solid
1 mg USD 132 In-stock
5 mg USD 240 In-stock
10 mg USD 420 In-stock
25 mg USD 756 In-stock
50 mg USD 1134 In-stock
100 mg USD 1580 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

MI-538 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

MI-538 is an inhibitor of the interaction between menin and MLL fusion proteins with an IC50 of 21 nM.

IC50 & Target

IC50 : 21 nM (menin and MLL interaction); Kd: 6.5 nM (menin)[1]
In Vitro

MI-538 inhibits the proliferation of MLL leukemia cells with a GI50 of 83 nM. MI-538 shows no effect (up to 6 μM) on growth of the control cell lines HL-60 and HM-2, which do not harbor MLL translocations, demonstrating good selectivity toward MLL fusion protein transformed cells. MI-538 binds to menin with low nanomolar affinity (Kd=6.5 nM). Its potent cellular activity originates from the improved binding affinity to menin and possibly increased cell membrane permeability. Treatment with MI-538 results in strong down regulation of expression of Hoxa9 and Meis1 genes. About 100 nM 27 was sufficient to reduce by ~50% Hoxa9 expression in MLL-AF9 cells, and even more pronounced effect was seen on Meis1 expression[1].

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

MI-538 Related Antibodies
In Vivo

Treatment with MI-538 results in a pronounced, about 80%, reduction in the MV4;11 tumor volume, without causing substantial signs of toxicity reflected by less than 10% reduction of the body weight. MI-538 demonstrates markedly improved exposure (area under the curve, AUC, values), Cmax (maximum compound concentration) in the blood plasma, and the lowest value of clearance. The half-life of MI-538 is about 1.6 h. MI-538 has also high oral bioavailability (~50%)[1].

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

566.60

Formula

C27H25F3N8OS
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC(F)(F)CC(S1)=CC2=C1N=CN=C2NC3CCN(CC4=C(O)C=C(N(CC5=CNN=C5)C(C#N)=C6)C6=C4)CC3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (176.49 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 1.7649 mL 8.8246 mL 17.6491 mL
5 mM 0.3530 mL 1.7649 mL 3.5298 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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: ≥ 10 mg/mL (17.65 mM); Clear solution

    This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 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% Corn Oil

    Solubility: ≥ 10 mg/mL (17.65 mM); Clear solution

    This protocol yields a clear solution of ≥ 10 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 (100.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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% 
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%
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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).
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: 98.67%

COA (248 KB) LCMS (268 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[1]

MOLM-13, MV4;11, HL-60 human leukemia cells as well as MLL-AF9 and HM-2 murine bone marrow cells are treated with MI-538 or 0.25% DMSO for 7 days. Media are changed at day 4 with viable cell number restored to the original concentration, and MI-538 are resupplied. An amount of 100 μL of cell suspension is transferred to 96-well plates for each sample in quadruplicates. Cell viability is measured using the MTT assay. Plates are read for absorbance at 570 nm[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice: Mice xenograft are randomly grouped with each group containing eight mice. Vehicle or MI-538 (45 mg/kg) are administrated once daily at designated doses using ip injections for 2 weeks. Body weight and tumor sizes are monitored three times a week[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7649 mL 8.8246 mL 17.6491 mL 44.1228 mL
5 mM 0.3530 mL 1.7649 mL 3.5298 mL 8.8246 mL
10 mM 0.1765 mL 0.8825 mL 1.7649 mL 4.4123 mL
15 mM 0.1177 mL 0.5883 mL 1.1766 mL 2.9415 mL
20 mM 0.0882 mL 0.4412 mL 0.8825 mL 2.2061 mL
25 mM 0.0706 mL 0.3530 mL 0.7060 mL 1.7649 mL
30 mM 0.0588 mL 0.2942 mL 0.5883 mL 1.4708 mL
40 mM 0.0441 mL 0.2206 mL 0.4412 mL 1.1031 mL
50 mM 0.0353 mL 0.1765 mL 0.3530 mL 0.8825 mL
60 mM 0.0294 mL 0.1471 mL 0.2942 mL 0.7354 mL
80 mM 0.0221 mL 0.1103 mL 0.2206 mL 0.5515 mL
100 mM 0.0176 mL 0.0882 mL 0.1765 mL 0.4412 mL
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MI-538 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:

MI-5381857417-10-7MI538MI 538Epigenetic Reader DomainInhibitorinhibitorinhibit

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