MZP-55
Based on 1 publication(s) in Google Scholar
MZP-55 is a BRD4 BD2 PROTAC degrader with a Kd value of 8 nM; its pDC50 values are 8.1 (short isoform) and 7.5 (long isoform), respectively. MZP-55 mediates the negatively cooperative formation of the Brd4BD2-VCB ternary complex, with Kd values of 109 nM and 183 nM for the VCB protein complex and the ternary complex, respectively. MZP-55 drives cMyc depletion and induces antiproliferative activity. MZP-55 can be used in the research of acute myeloid leukemia.
(Pink: BRD4 BD2 ligand (HY-13960); Blue: VHL ligand (HY-125845); Black: linker (HY-130524)).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.94%
- CAS 番号: 2010159-48-3
- 分子式: C57H70ClN7O10S
- 分子量:1080.72
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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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HY-112376
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dBET6PROTAC BET Degrader -
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MedChemExpress（MCE）の使用を引用している文献 MZP-55
MorePROTACs アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
[1]|
BRD4 BD2 8 nM (Kd) |
VHL |
BRD3 |
体外実験
MZP-55 (50 nM; 4 h) reduces the protein levels of Brd4 and cMyc in MV4;11 and HL60 acute myeloid leukemia cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:acute myeloid leukemia MV4;11 cells
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Concentration:50 nM
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Incubation Time:4 h
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Result:Induced 81% depletion of Brd4 relative to vehicle control.
Induced 60% depletion of cMyc relative to vehicle control.
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Cell Line:acute myeloid leukemia HL60 cells
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Concentration:50 nM
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Incubation Time:4 h
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Result:Induced 22% depletion of Brd4 relative to vehicle control.
Induced 47% depletion of cMyc relative to vehicle control.
化学情報
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CAS 番号 2010159-48-3
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性状 Solid
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分子量 1080.72
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分子式 C57H70ClN7O10S
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Color White to off-white
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SMILES
CC(N=CS1)=C1C2=CC=C(CNC([C@@H]3C[C@@H](O)CN3C([C@H](C(C)(C)C)NC(COCCOCCOCCOCCNC(C(C=C4)=CC=C4C5=CC6=C(C=C5)N(C(C)=O)[C@@H](C)C[C@H]6NC7=CC=C(Cl)C=C7)=O)=O)=O)=O)C=C2
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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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Structure
PROTAC-mediated activation, rather than degradation, of a nuclear receptor reveals complex ligand-receptor interaction network. [Abstract]2024 Dec 5;32(12):2352-2363.e8. PMID: 39389062
溶剤 & 溶解度
体外:
DMSO : 50 mg/mL (46.27 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: ≥ 2.5 mg/mL (2.31 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.
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 (274 KB)
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SDS (396 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Chan KH, et al. Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds. Journal of medicinal chemistry. 2018 Jan 25;61(2):504-513. [Content Brief]
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 |
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| DMSO | 1 mM | 0.9253 mL | 4.6265 mL | 9.2531 mL | 23.1327 mL |
| 5 mM | 0.1851 mL | 0.9253 mL | 1.8506 mL | 4.6265 mL | |
| 10 mM | 0.0925 mL | 0.4627 mL | 0.9253 mL | 2.3133 mL | |
| 15 mM | 0.0617 mL | 0.3084 mL | 0.6169 mL | 1.5422 mL | |
| 20 mM | 0.0463 mL | 0.2313 mL | 0.4627 mL | 1.1566 mL | |
| 25 mM | 0.0370 mL | 0.1851 mL | 0.3701 mL | 0.9253 mL | |
| 30 mM | 0.0308 mL | 0.1542 mL | 0.3084 mL | 0.7711 mL | |
| 40 mM | 0.0231 mL | 0.1157 mL | 0.2313 mL | 0.5783 mL |
MZP-55 関連分類
HY-112377 関連分類
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