BRD9876
Based on 1 publication(s) in Google Scholar
BRD9876 is the “rigor” inhibitor that locks kinesin-5 (Eg5) in a state with enhanced microtubules (MTs) binding, leading to bundling and stabilization of MTs. BRD9876 interacts with the tyrosine 104 residue that is part of the α4-α6 allosteric binding pocket. BRD9876 specifically targets microtubule-bound Eg5 and selectively inhibits myeloma over CD34 cells. BRD9876 has the potential for multiple myeloma (MM) research.
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- 純度: 99.37%
- CAS 番号: 32703-82-5
- 分子式: C16H14N2
- 分子量:234.30
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保管条件:
Store at room temperature, keep dry and cool.
In solvent -80°C, 1 year , -20°C, 6 months
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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
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 BRD9876
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生物活性
BRD9876 (10 μM; 24 hours) reveales rapid arrest of cells at the G2/M phase starting as early as 2h of treatment in MM1S cells[1].
BRD9876 exhibits approximately 3-fold selectivity for MM1S myeloma cells (IC50=3.1 μM) over CD34+ derived hematopoietic cells (IC50=9.1 μM)[1].
BRD9876 (0.1, 1, 10, 100 uM) is able to overcome, in MM1S cells, stromal resistance of bone marrow stromal cells (BMSCs) from MM bone marrow aspirates but only minimal effects are observed with BRD9876 against primary MM cells[1].
BRD9876 is completely ineffective at inhibiting the basal ATPase activity of Eg5, in contrast to loop L5-binding monastrol or α4/α6-binding BI8 which shows greater activity against basal Eg5 ATPase activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MM1S cells and CD34 hematopoietic cells
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Concentration:10 μM
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Incubation Time:24 hours
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Result:Revealed rapid arrest of cells at the G2/M phase starting as early as 2h of treatment in MM1S cells.
Showed markedly less G2/M arrest in CD34 hematopoietic cells.
化学情報
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CAS 番号 32703-82-5
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性状 Solid
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分子量 234.30
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分子式 C16H14N2
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Color Light yellow to yellow
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SMILES
CC(C)(C1=CC2=CC(C#N)=C(C#N)C=C2C=C1)C
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Store at room temperature, keep dry and cool
In solvent -80°C 1 year -20°C 6 months
Publications (1)
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Journal Impact Factor
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Most Recent
溶剤 & 溶解度
DMF : 1 mg/mL (4.27 mM; ultrasonic and warming and heat to 60°C)
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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.
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.
Working solution concentration: 0.22 mg/mL
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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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Shrikanta Chattopadhyay, et al. Niche-Based Screening in Multiple Myeloma Identifies a Kinesin-5 Inhibitor with Improved Selectivity over Hematopoietic Progenitors. Cell Rep. 2015 Feb 10;10(5):755-770. [Content Brief]
[2]. Chieh-Ting Fang, et al. HSP70 regulates Eg5 distribution within the mitotic spindle and modulates the cytotoxicity of Eg5 inhibitors. Cell Death Dis. 2020 Sep 1;11(8):715. [Content Brief]
[3]. Anke Maes, et al. The therapeutic potential of cell cycle targeting in multiple myeloma. Oncotarget. 2017 Jun 28;8(52):90501-90520. [Content Brief]
[4]. Geng-Yuan Chen, et al. Eg5 Inhibitors Have Contrasting Effects on Microtubule Stability and Metaphase Spindle Integrity. ACS Chem Biol. 2017 Apr 21;12(4):1038-1046. [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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMF | 1 mM | 4.2680 mL | 21.3402 mL | 42.6803 mL | 106.7008 mL |
BRD9876 関連分類
HY-110208 関連分類
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