KS15
Based on 3 publication(s) in Google Scholar
KS15 is an inhibitor of the interactions between cryptochromes (CRYs: CRY1 and CRY2) and the CLOCK:BMAL1 heterodimer. KS15 impairs the feedback actions of CRYs on E-box-dependent transcription (EC50=4.9 μM) by CLOCK:BMAL1 heterodimer, an indispensable transcriptional regulator of the mammalian circadian clock. Anti-proliferative activity.
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- 純度: 99.46%
- CAS 番号: 1033781-20-2
- 分子式: C20H22BrNO4
- 分子量:420.30
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保管条件:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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 KS15
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生物活性
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CRY1 |
Applications of KS15 at different concentrations from 1 μM to 10 μM restored the E-box-driven luciferase activities in a dose-dependent manner, indicating that KS15 evidently impairs the suppressive actions of CRYs on CLOCK:BMAL1-induced transcription. KS15 inhibits the interactions between CRYs and BMAL1, resulting in the enhanced transcriptional activity in the core loop of the molecular circadian clock[1].
KS15 directly binds to the C-terminal region of cryptochromes (CRYs: CRY1 and CRY2) and enhances E-box-mediated transcription[2].
KS15 decreases the speed of cell growth and increased the chemosensitivity of MCF-7 cells to Doxorubicin and Tamoxifen. KS15 exerts an anti-proliferative effect and increases sensitivity to anti-tumor drugs in a specific type of breast cancer[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 1033781-20-2
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性状 Solid
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分子量 420.30
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分子式 C20H22BrNO4
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Color White to off-white
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SMILES
CCO[C@@H](C(O)=O)CC1=CC(/C(C)=N/OCC2=CC=C(C=C2)Br)=CC=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (3)
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Journal Impact Factor
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Most Recent
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Neurosci Bull
Agomelatine Targets Aquaporin-4 Polarization to Rescue Glymphatic Dysfunction in Parkinson's Disease. [Abstract]2025 Nov 18. PMID: 41251938 -
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溶剤 & 溶解度
DMSO : 100 mg/mL (237.93 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (5.95 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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 (5.95 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 (272 KB)
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SDS (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Chun SK, et al. A synthetic cryptochrome inhibitor induces anti-proliferative effects and increases chemosensitivity in human breast cancer cells. Biochem Biophys Res Commun. 2015;467(2):441-446. [Content Brief]
[2]. Jang J, et al. The cryptochrome inhibitor KS15 enhances E-box-mediated transcription by disrupting the feedback action of a circadian transcription-repressor complex. Life Sci. 2018;200:49-55. [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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3793 mL | 11.8963 mL | 23.7925 mL | 59.4813 mL |
| 5 mM | 0.4759 mL | 2.3793 mL | 4.7585 mL | 11.8963 mL | |
| 10 mM | 0.2379 mL | 1.1896 mL | 2.3793 mL | 5.9481 mL | |
| 15 mM | 0.1586 mL | 0.7931 mL | 1.5862 mL | 3.9654 mL | |
| 20 mM | 0.1190 mL | 0.5948 mL | 1.1896 mL | 2.9741 mL | |
| 25 mM | 0.0952 mL | 0.4759 mL | 0.9517 mL | 2.3793 mL | |
| 30 mM | 0.0793 mL | 0.3965 mL | 0.7931 mL | 1.9827 mL | |
| 40 mM | 0.0595 mL | 0.2974 mL | 0.5948 mL | 1.4870 mL | |
| 50 mM | 0.0476 mL | 0.2379 mL | 0.4759 mL | 1.1896 mL | |
| 60 mM | 0.0397 mL | 0.1983 mL | 0.3965 mL | 0.9914 mL | |
| 80 mM | 0.0297 mL | 0.1487 mL | 0.2974 mL | 0.7435 mL | |
| 100 mM | 0.0238 mL | 0.1190 mL | 0.2379 mL | 0.5948 mL |
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