Art. -Nr.: HY-15222

Menin-MLL inhibitor MI-2

4 Cited Publications

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Based on 4 publication(s) in Google Scholar

Menin-MLL inhibitor MI-2 is a competitive and selective Menin-MLL interaction inhibitor with an IC₅₀ value of 446 nM and a K_i value of 158 nM. Menin-MLL inhibitor MI-2 downregulates the expression of target genes such as HOXA9 and MEIS1, inhibits proliferation of leukemia cells and induces apoptosis and differentiation. Menin-MLL inhibitor MI-2 is proming for rasearch of MLL-rearranged acute leukemias (e.g., AML, ALL).

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Reinheit: 99.41%
CAS. Nr.: 1271738-62-5
Formel: C₁₈H₂₅N₅S₂
Molecular Weight:375.55

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Menin-MLL inhibitor MI-2 Chemical Structure

CAS. Nr.: 1271738-62-5

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 446±28 nM (Menin-MLL)^[1]

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Cellular Effect

Cell Line	Type	Value	Description	References
HL-60	IC₅₀	>10 μM Compound: 1; MI-2	Antiproliferative activity against human HL-60 cells harboring MLL-AF4 assessed as cell growth inhibition measured for 72 hrs by MTT assay Antiproliferative activity against human HL-60 cells harboring MLL-AF4 assessed as cell growth inhibition measured for 72 hrs by MTT assay	[PMID: 36173787]
HL-60	IC₅₀	>10 μM Compound: 7; MI-2	Antiproliferative activity against human HL-60 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human HL-60 cells incubated for 72 hrs by MTT assay	[PMID: 38367493]
MV4-11	GI₅₀	9.5 μM Compound: 1; MI-2	Antiproliferative activity against human MV4-11 cells Antiproliferative activity against human MV4-11 cells	[PMID: 34726905]
MV4-11	IC₅₀	7.62 μM Compound: 1; MI-2	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured for 3 days followed by replacement with fresh medium of compound and measured after 72 hrs by cell counting assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured for 3 days followed by replacement with fresh medium of compound and measured after 72 hrs by cell counting assay	[PMID: 36173787]
MV4-11	IC₅₀	8.52 μM Compound: 1; MI-2	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured for 3 days by cell counting assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured for 3 days by cell counting assay	[PMID: 36173787]
MV4-11	IC₅₀	9.2 μM Compound: 1; MI-2	Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 assessed as cell growth inhibition measured for 72 hrs by MTT assay Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 assessed as cell growth inhibition measured for 72 hrs by MTT assay	[PMID: 36173787]
MV4-11	IC₅₀	9.2 μM Compound: 7; MI-2	Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by MTT assay	[PMID: 38367493]

In Vitro

Menin-MLL inhibitor MI-2 very effectively blocks proliferation of MLL-AF9 and MLL-ENL transduced BMC, with GI₅₀ values of about 5 μM. Assessment of diverse hydrophobic groups at R1 led to the development of several compounds with IC₅₀ values in the nanomolar range, including MI-2 (IC₅₀= 446±28 nM) and MI-3 (IC₅₀=648±25 nM).The dissociation constants measured for the menin-MLL inhibitors are at the nanomolar level, K_d=158 nM for MI-2. MI-2 can access the protein target and very effectively inhibit the menin-MLL-AF9 interaction in human cells. Furthermore, MI-2 shows only a small effect on the cell growth of E2A-HLF transduced BMC (GI₅₀>50 μM), which may be due to inhibition of the menin interaction with wild-type MLL. Treatment with MI-2 results in GI₅₀ values below 10 μM in MV4;11 (harboring MLL-AF4; GI₅₀=9.5 μM), KOPN-8 (MLL-ENL; GI₅₀=7.2 μM) and ML-2 (MLL-AF6; GI₅₀=8.7 μM), and in MonoMac6 (MLL-AF9; GI₅₀=18 μM)^[1].

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

Chemical Information

CAS. Nr. 1271738-62-5
Appearance Solid
Molecular Weight 375.55
Formel C₁₈H₂₅N₅S₂
Color Light yellow to yellow
SMILES

CCCC1=CC2=C(N3CCN(C4=NCC(C)(C)S4)CC3)N=CN=C2S1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (4)

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Journal Impact Factor

Cell Syst

A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]

2018 Apr 25;6(4):424-443.e7. PMID: 29655704
Molecules

Modulatory Effect of Curcumin on Expression of Methyltransferase/Demethylase in Colon Cancer Cells: Impact on wt p53, mutp53 and c-Myc. [Abstract]

2025 Jul 22;30(15):3054. PMID: 40807229
Oncol Lett

Mucosa‑associated lymphoid tissue lymphoma translocation protein 1 inhibitor, MI‑2, attenuates non‑small cell lung cancer cell proliferation, migration and invasion, and promotes apoptosis by suppressing the JNK/c‑JUN pathway. [Abstract]

2024 Jul 30;28(4):465. PMID: 39119234
Patent

US20180263995A1.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (133.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6628 mL

13.3138 mL

26.6276 mL

5 mM

0.5326 mL

2.6628 mL

5.3255 mL

10 mM

0.2663 mL

1.3314 mL

2.6628 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 (6.66 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.66 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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.66 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

Cell Assay^[1]

5×10⁵ HEK 293 cells/mL are plated in 12-well plates (1 mL/well) and treated with compounds (e.g., MI-2) (0.25% final concentration of DMSO for each condition) or 0.25% DMSO control and incubated for 48h at 37°C in a 5% CO₂ incubator. After incubation, 1.5×10⁵ cells are harvested and resuspended in 100 μL 1× Annexin V binding buffer from the Annexin V-FITC Apoptosis kit, incubated with 4 μL of AnnexinV-FITC and 6 μL of Propidium iodide at room temperature in the dark for 10 minutes and analyzed by flow cytometry on a LSR II instrument. Data analysis is performed using WinList software. The experiments are performed three times in triplicates with calculation of mean and standard deviation for each condition^[1].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Grembecka J, et al. Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia. Nature Chemical Biology (2012), 8(3), 277-284. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.6628 mL	13.3138 mL	26.6276 mL	66.5690 mL
	5 mM	0.5326 mL	2.6628 mL	5.3255 mL	13.3138 mL
	10 mM	0.2663 mL	1.3314 mL	2.6628 mL	6.6569 mL
	15 mM	0.1775 mL	0.8876 mL	1.7752 mL	4.4379 mL
	20 mM	0.1331 mL	0.6657 mL	1.3314 mL	3.3285 mL
	25 mM	0.1065 mL	0.5326 mL	1.0651 mL	2.6628 mL
	30 mM	0.0888 mL	0.4438 mL	0.8876 mL	2.2190 mL
	40 mM	0.0666 mL	0.3328 mL	0.6657 mL	1.6642 mL
	50 mM	0.0533 mL	0.2663 mL	0.5326 mL	1.3314 mL
	60 mM	0.0444 mL	0.2219 mL	0.4438 mL	1.1095 mL
	80 mM	0.0333 mL	0.1664 mL	0.3328 mL	0.8321 mL
	100 mM	0.0266 mL	0.1331 mL	0.2663 mL	0.6657 mL

Keywords

Menin-MLL inhibitor MI-2

4 Cited Publications

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Menin-MLL inhibitor MI-2

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Publications Citing Use of MedChemExpress (MCE) Menin-MLL inhibitor MI-2

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Menin-MLL inhibitor MI-2

Apoptosis Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Anti-Blood Cancer Compound Library

Protein-protein Interaction Inhibitor Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Menin-MLL inhibitor MI-2

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Menin-MLL inhibitor MI-2 Related Classifications

HY-15222 Related Classifications