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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.21%
- No. CAS: 3029584-84-4
- Fòrmula: C20H15N3O2
- Peso molecular:329.35
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
[1]|
NEK1 11.5 nM (IC50) |
In Vitro
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.
In Vivo
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.
Chemical Information
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No. CAS 3029584-84-4
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Appearance Solid
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Peso molecular 329.35
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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.
Pureza y Documentación
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Ficha de datos (282 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 Related Classifications
HY-144425 Related Classifications
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