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^[1].

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.

544.54

C₂₇H₂₈F₄N₆O₂

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Wang L, et, al. Discovery of novel biaryl urea derivatives against IL-1β release with low toxicity based on NEK7 inhibitor. Eur J Med Chem. 2024 Dec 3:283:117125.  [Content Brief]