MI-3
Based on 1 publication(s) in Google Scholar
MI-3 (Menin-MLL inhibitor 3) is a potent and high affinity menin-MLL inhibitor with an IC50 of 648 nM and a Kd of 201 nM.
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- 純度: 99.58%
- CAS 番号: 1271738-59-0
- 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
MedChemExpress(MCE)の使用を引用している文献 MI-3
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生物活性
製品説明
IC50 & Target
IC50: 648 nM (menin-MLL); Kd: 201 nM (menin-MLL)[1]
体外実験
MI-3 (12.5-50 μM; HEK293 cells) treatment effectively inhibits the menin-MLL-AF9 interaction in human cells[1].
MI-3 (0-1.6 μM; 72 hours; KOPN-8 and MV4;11 cells) treatment shows an effective and dose-dependent growth inhibition in KOPN-8, MV4 and ME-1 cells[1].
MI-3 (12.5-50 μM; 48 hours; MV4;11 cells) treatment results in a substantial, and dose-dependent increase in Annexin V and AnnexinV/propidium iodide (PI) cells, demonstrating an increase in the number of cells undergoing apoptosis[1].
MI-3 (6.25-25 μM; 6 days; THP-1 cells) treatment results in substantially reduced expression of HOXA9 and MEIS1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293 cells
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Concentration:12.5 μM, 25 μM, 50 μM
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Incubation Time:
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Result:Very effectively inhibited the menin-MLL-AF9 interaction in human cells.
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Cell Line:KOPN-8 and MV4;11 cells
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Concentration:0 μM, 0.4 μM, 0.8 μM, 1.2 μM, 1.6 μM
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Incubation Time:72 hours
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Result:Showed an effective and dose-dependent growth inhibition in KOPN-8 and MV4;11 cells.
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Cell Line:MV4;11 cells
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Concentration:12.5 μM, 25 μM, 50 μM
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Incubation Time:48 hours
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Result:Resulted in an increase in the number of cells undergoing apoptosis.
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Cell Line:THP-1 cells
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Concentration:6.25 μM, 12.5 μM, 25 μM
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Incubation Time:6 days
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Result:Resulted in substantially reduced expression of HOXA9 and MEIS1.
化学情報
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CAS 番号 1271738-59-0
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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
CC(C)C1=CC2=C(N3CCN(C4=NCC(C)(C)S4)CC3)N=CN=C2S1
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別名
Menin-MLL inhibitor 3
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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 (1)
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Journal Impact Factor
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Most Recent
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Clin Transl Med
Loss of MEN1 leads to renal fibrosis and decreases HGF-Adamts5 pathway activity via an epigenetic mechanism. [Abstract]2022 Aug;12(8):e982. PMID: 35968938
溶剤 & 溶解度
体外:
DMSO : 8.33 mg/mL (22.18 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)
体内:
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: ≥ 0.83 mg/mL (2.21 mM); Clear solution
This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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: ≥ 0.83 mg/mL (2.21 mM); Clear solution
This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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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%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.
純度とドキュメンテーション
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データシート (275 KB)
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SDS (252 KB)
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- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 |