Menin-MLL inhibitor MI-2
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 Ki 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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- 純度: 99.41%
- CAS 番号: 1271738-62-5
- 分子式: C18H25N5S2
- 分子量:375.55
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Menin-MLL inhibitor MI-2
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生物活性
IC50: 446±28 nM (Menin-MLL)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HL-60 | IC50 |
>10 μM
Compound: 1; MI-2
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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
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[PMID: 36173787] |
| HL-60 | IC50 |
>10 μM
Compound: 7; MI-2
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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
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[PMID: 38367493] |
| MV4-11 | GI50 |
9.5 μM
Compound: 1; MI-2
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Antiproliferative activity against human MV4-11 cells
Antiproliferative activity against human MV4-11 cells
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[PMID: 34726905] |
| MV4-11 | IC50 |
7.62 μM
Compound: 1; MI-2
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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
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[PMID: 36173787] |
| MV4-11 | IC50 |
8.52 μM
Compound: 1; MI-2
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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
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[PMID: 36173787] |
| MV4-11 | IC50 |
9.2 μM
Compound: 1; MI-2
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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
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[PMID: 36173787] |
| MV4-11 | IC50 |
9.2 μM
Compound: 7; MI-2
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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
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[PMID: 38367493] |
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, Kd=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.
化学情報
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CAS 番号 1271738-62-5
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性状 Solid
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分子量 375.55
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分子式 C18H25N5S2
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Color Light yellow to yellow
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SMILES
CCCC1=CC2=C(N3CCN(C4=NCC(C)(C)S4)CC3)N=CN=C2S1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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
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Most Recent
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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 -
溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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 (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.
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 (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.
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.
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.
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.
プロトコル
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.
純度とドキュメンテーション
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データシート (276 KB)
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取扱説明書 (2659 KB)
参考文献
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 | 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 |
Menin-MLL inhibitor MI-2 関連分類
HY-15222 関連分類
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