NEK7-IN-2
NEK7-IN-2 is a NEK7 inhibitor. NEK7-IN-2 increases the thermal stability of NEK7, disrupts the NEK7-NLRP3 interaction, inhibits NLRP3 inflammasome assembly, and suppresses the release of IL-1β (with an IC50 of 0.048 μM against IL-1β). NEK7-IN-2 can be used for the research of inflammatory diseases.
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- Formule: C27H28F4N6O2
- Masse moléculaire:544.54
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
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Help & FAQs
Activité biologique
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IL-1β 0.048 μM (IC50) |
NEK7 |
NLRP3 |
NEK7-IN-2 (Compound 23) (0.1 μM; 2-4 h) potently inhibits IL-1β release in mouse bone marrow-derived macrophages with an IC50 of 0.048 μM and low cytotoxicity, achieving a high selectivity index of 80.32[1].
NEK7-IN-2 (compound 23) binds directly to NEK7 in mouse bone marrow-derived macrophages, increasing the protein's thermal stability[1].
NEK7-IN-2 (compound 23) blocks the interaction between NLRP3 and NEK7 in mouse bone marrow-derived macrophages, inhibiting NLRP3 inflammasome assembly[1].
NEK7-IN-2 (compound 23) binds to NEK7 (PDB: 6s76) via critical interactions with residues including R121, which disrupts the NLRP3-NEK7 interaction interface[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:mouse bone marrow-derived macrophages (BMDMs)
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Concentration:0.1 μM (IL-1β inhibition assay; cytotoxicity assay); dose-dependent concentrations (IC50/CC50 determination)
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Incubation Time:2 h (IL-1β inhibition assay); 4 h (cytotoxicity assay)
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Result:Inhibited IL-1β release by 90.26%.
Maintained 98.33% cell viability.
Exhibited an IL-1β inhibition IC50 of 0.048 μM and a cytotoxicity CC50 of 3.842 μM, resulting in a selectivity index (SI) of 80.32.
Chemical Information
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Masse moléculaire 544.54
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Formule C27H28F4N6O2
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SMILES
FC1=C(NC(NC2=CC(C(F)(F)F)=C(CN3CCN(C)CC3)C=C2)=O)C=CC(C4=CC=C(NC(C)=O)N=C4)=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NEK7-IN-2 Related Classifications
HY-168737 Related Classifications
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