NEK7 degrader-2

NEK7 degrader-2 (compound 25) (1 μM; 25°C; 30 min) promotes the formation of the NEK7-compound-CRBN/DDB1 ternary complex in an AlphaLISA assay containing 200 nM biotinylated NEK7 and 200 nM 6×His-CRBN/Strep-DDB1, with a normalized ternary-complex activity of >80% at 1 μM^[1].
NEK7 degrader-2 (25°C; 180 min) induces the formation of the NEK7-compound-CRBN/DDB1 ternary complex in an HTRF assay containing 24 nM NEK7 and 52.8 nM 6×His-CRBN/Strep-DDB1, with an HTRF pEC₅₀ rating of +++, corresponding to 6.0 < pEC₅₀ < 6.5^[1].
NEK7 degrader-2 (0.1-10 μM; 24 h) reduces NEK7-HiBiT protein in HEK293 cells stably expressing NEK7-HiBiT; at 10 μM, the NEK7-HiBiT protein level decreases to ≤25% of the DMSO control^[1].
NEK7 degrader-2 (0.1-10 μM; 24 h) reduces endogenous NEK7 protein levels in a dose-dependent manner in human PBMC-derived macrophages; at 10 μM, NEK7 protein levels decrease to ≤10% of the DMSO control, while the β-actin and vinculin loading controls remain relatively stable^[1].
After preincubation with NEK7 degrader-2 (0.1-10 μM; 24 h) in human PBMC-derived macrophages, followed by NLRP3 inflammasome activation via LPS (1 μg/mL; 3 h) priming and Nigericin (HY-127019) (5 μM; 1 h), IL-1β release is reduced^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.