BSc5367
Based on 1 Customer Validation
BSc5367 is a NEK1 kinase inhibitor with an IC50 of 11.5 nM. BSc5367 modulates the cell cycle, DNA repair, and microtubule dynamics, reduces YAP1 phosphorylation, induces DNA damage, and upregulates γH2A.X. BSc5367 drives TDP-43 nucleocytoplasmic translocation, inhibits NEK1-mediated ETS1 phosphorylation, increases ETS1 acetylation, sensitizes ccRCC cells to Sunitinib (HY-10255A), and mimics the phenotype of NEK1-mutant motor neurons. BSc5367 inhibits NEK1 in zebrafish models and causes expansion of renal tubule volume, affecting pronephros development. BSc5367 can be used in research related to polycystic kidney disease, renal cancer, and amyotrophic lateral sclerosis.
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 : 98.21%
- CAS 番号: 3029584-84-4
- 分子式: C20H15N3O2
- 分子量:329.35
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
生物活性
製品説明
IC50 & Target
[1]|
NEK1 11.5 nM (IC50) |
体外実験
BSc5367 (1 μM) shows low A-B permeability (0.13 × 10-6 cm/s) and B-A permeability (0.04 × 10-6 cm/s) in Caco-2 cells[1].
BSc5367 (11.5 nM; 48 h) inhibits NEK1 in human motor neurons, reducing kinase activity and YAP1 pTyr407 while increasing γH2A.X and inducing TDP-43 nucleocytoplasmic translocation[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:786-O, ACHN, and 786-O sunitinib-resistant (786-O R) ccRCC cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Sensitized 786-O, ACHN, and 786-O R ccRCC cells to Sunitinib in CCK-8 assays.
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Cell Line:786-O and ACHN ccRCC cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Increased ETS1-K245 acetylation in 786-O and ACHN cells.
Decreased ETS1 phosphorylation in 786-O cells.
Co-IP showed increased ETS1 acetylation with reduced HIF-2α association.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:wild-type (embryos/larvae at 4-96 h post fertilization (hpf))[1]
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Dosage:0.5 µM
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Administration:immersion; continuous incubation from 4 hpf to 96 h
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Result:Caused an increase in fluorescence intensity and minor tubular volume expansion in the developing zebrafish pronephros.
化学情報
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CAS 番号 3029584-84-4
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性状 Solid
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分子量 329.35
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分子式 C20H15N3O2
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Color White to yellow
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SMILES
COC(C1=CC(C2=CN=C3NC=C(C3=C2)C4=CN=CC=C4)=CC=C1)=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 6 months -20°C 1 month
溶剤 & 溶解度
体外:
DMSO : 10 mg/mL (30.36 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, 6 months; -20°C, 1 month. 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. 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)
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: ≥ 1 mg/mL (3.04 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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: 1 mg/mL (3.04 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1 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 (10.0 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.
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 (282 KB)
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SDS (251 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, 6 months; -20°C, 1 month. 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 |
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| DMSO | 1 mM | 3.0363 mL | 15.1814 mL | 30.3628 mL | 75.9071 mL |
| 5 mM | 0.6073 mL | 3.0363 mL | 6.0726 mL | 15.1814 mL | |
| 10 mM | 0.3036 mL | 1.5181 mL | 3.0363 mL | 7.5907 mL | |
| 15 mM | 0.2024 mL | 1.0121 mL | 2.0242 mL | 5.0605 mL | |
| 20 mM | 0.1518 mL | 0.7591 mL | 1.5181 mL | 3.7954 mL | |
| 25 mM | 0.1215 mL | 0.6073 mL | 1.2145 mL | 3.0363 mL | |
| 30 mM | 0.1012 mL | 0.5060 mL | 1.0121 mL | 2.5302 mL |
BSc5367 関連分類
HY-144425 関連分類
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