NEK7 degrader-1
Based on 1 Customer Validation
NEK7 degrader-1 is a NEK7 molecular glue degrader with a DC50 of 9 nM. NEK7 degrader-1 dose-dependently inhibits caspase-1 activity and IL-Ιβ release in macrophages in response to NLRP3 inflammasome activation. NEK7 degrader-1 can be used for autoinflammatory and autoimmune disorders like multiple sclerosis, neurodegeneraive diseases like Alzheimer's disease and cardiovascular and melabolic disorders like pericarditis and Type 2 diabetes research.
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- Pureté : 99.94%
- CAS No.: 3069891-91-1
- Formule: C21H22Cl2N4O3
- Masse moléculaire:449.33
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Stockage:Powder -20°C, 3 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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
Caspase-1 |
IL-1β |
NEK7 9 nM (DC50) |
NLRP3 inflammasome |
In Vitro
NEK7 degrader-1 (Compound 14) dose-dependently inhibits caspase-1 activity (IC50 of 1.85 nM) and IL-Ιβ release (IC50 of 1.95 nM) in macrophages in response to NLRP3 inflammasome activation[1].
NLRP3 modulator 8 (Compound 14) binds to CRBN by HTRF assay with an EC50 value of 0.11μM
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3069891-91-1
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Appearance Solid
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Masse moléculaire 449.33
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Formule C21H22Cl2N4O3
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Color White to off-white
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SMILES
O=C1NC(C(CC1)C2=C(C=C(CNC(C(C)(C)C3=NC=C(C)C=N3)=O)C=C2Cl)Cl)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (222.55 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 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.
Working solution concentration: 0.22 mg/mL
Pureté et documentation
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Fiche technique (271 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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Instruction de manipulation (2659 KB)
Références
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2255 mL | 11.1277 mL | 22.2554 mL | 55.6384 mL |
| 5 mM | 0.4451 mL | 2.2255 mL | 4.4511 mL | 11.1277 mL | |
| 10 mM | 0.2226 mL | 1.1128 mL | 2.2255 mL | 5.5638 mL | |
| 15 mM | 0.1484 mL | 0.7418 mL | 1.4837 mL | 3.7092 mL | |
| 20 mM | 0.1113 mL | 0.5564 mL | 1.1128 mL | 2.7819 mL | |
| 25 mM | 0.0890 mL | 0.4451 mL | 0.8902 mL | 2.2255 mL | |
| 30 mM | 0.0742 mL | 0.3709 mL | 0.7418 mL | 1.8546 mL | |
| 40 mM | 0.0556 mL | 0.2782 mL | 0.5564 mL | 1.3910 mL | |
| 50 mM | 0.0445 mL | 0.2226 mL | 0.4451 mL | 1.1128 mL | |
| 60 mM | 0.0371 mL | 0.1855 mL | 0.3709 mL | 0.9273 mL | |
| 80 mM | 0.0278 mL | 0.1391 mL | 0.2782 mL | 0.6955 mL | |
| 100 mM | 0.0223 mL | 0.1113 mL | 0.2226 mL | 0.5564 mL |
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