BTB-1
Based on 2 publication(s) in Google Scholar
BTB-1 is a potent, selective and reversible mitotic motor protein Kif18A inhibitor with an IC50 of 1.69 μM.
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- 純度: 99.91%
- CAS 番号: 86030-08-2
- 分子式: C12H8ClNO4S
- 分子量:297.71
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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
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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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MedChemExpress（MCE）の使用を引用している文献 BTB-1
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生物活性
IC50: 1.69 μM (Kif18A)[1]
BTB-1 blocks the motility of Kif18A in a reversible manner. BTB-1 inhibits Kif18A in an adenosine triphosphate (ATP)-competitive but microtubule-uncompetitive manner and slows down the progression of cells through mitosis. 100 μM BTB-1 does not significantly inhibit any of the other tested mitotic kinesins. BTB-1 competes with ATP for Kif18A binding only when the motor-protein is associated with its pseudosubstrate microtubules. HeLa cells treated with BTB-1 accumulate in mitosis in a dose-dependent manner[1]. BTB-1 shows cell toxicity with an EC50 values of 35.8 μM. HeLa cells treated with 50 μM BTB-1 reveals severe defects in spindle morphology and chromosome alignment. Treatment with high concentrations of BTB-1 does not result in elongated spindles[2].
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 86030-08-2
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性状 Solid
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分子量 297.71
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分子式 C12H8ClNO4S
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Color White to off-white
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SMILES
O=S(C1=CC=C(Cl)C=C1[N+]([O-])=O)(C2=CC=CC=C2)=O
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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 (2)
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Journal Impact Factor
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Most Recent
溶剤 & 溶解度
DMSO : ≥ 100 mg/mL (335.90 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (8.40 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 (8.40 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
BTB-1 is prepared in DMSO. The activity of His-Kif18Amotor at increasing concentrations of ATP is monitored in the presence of 3 μM Mts and increasing concentrations of BTB-1 (0.21 μM, 0.42 μM, 0.85 μM, 1.7 μM) or DMSO as control[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 (279 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Catarinella M, et al. BTB-1: a small molecule inhibitor of the mitotic motor protein Kif18A. Angew Chem Int Ed Engl. 2009;48(48):9072-6. [Content Brief]
[2]. Braun J, et al. Synthesis and biological evaluation of optimized inhibitors of the mitotic kinesin Kif18A. ACS Chem Biol. 2015 Feb 20;10(2):554-60. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.3590 mL | 16.7949 mL | 33.5897 mL | 83.9743 mL |
| 5 mM | 0.6718 mL | 3.3590 mL | 6.7179 mL | 16.7949 mL | |
| 10 mM | 0.3359 mL | 1.6795 mL | 3.3590 mL | 8.3974 mL | |
| 15 mM | 0.2239 mL | 1.1197 mL | 2.2393 mL | 5.5983 mL | |
| 20 mM | 0.1679 mL | 0.8397 mL | 1.6795 mL | 4.1987 mL | |
| 25 mM | 0.1344 mL | 0.6718 mL | 1.3436 mL | 3.3590 mL | |
| 30 mM | 0.1120 mL | 0.5598 mL | 1.1197 mL | 2.7991 mL | |
| 40 mM | 0.0840 mL | 0.4199 mL | 0.8397 mL | 2.0994 mL | |
| 50 mM | 0.0672 mL | 0.3359 mL | 0.6718 mL | 1.6795 mL | |
| 60 mM | 0.0560 mL | 0.2799 mL | 0.5598 mL | 1.3996 mL | |
| 80 mM | 0.0420 mL | 0.2099 mL | 0.4199 mL | 1.0497 mL | |
| 100 mM | 0.0336 mL | 0.1679 mL | 0.3359 mL | 0.8397 mL |
BTB-1 関連分類
HY-101770 関連分類
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