Fig. 1
From: NF-κB inducing kinase is a therapeutic target for systemic lupus erythematosus
NIK SMI1 is a highly selective and potent inhibitor of NIK. a Structure of NIK SMI1 b Model of NIK SMI1 (orange) docked into the 4G3E crystal structure. The interaction surface around the ligand is depicted in blue and hydrogen bond contacts are in green. c Inhibition of human NIK enzymatic activity by SMI1. A representative curve is shown, and the calculated Ki represents the mean ± standard deviation of two independent experiments. d, e Inhibition of anti-LTβR induced non-canonical (d) and TNF induced canonical (e) signaling by NIK SMI1. We show representative images of p100/p52 (d) or RelA (e) in turquoise and nuclear staining for DRAQ5 in red (scale bar = 100 μm), and calculated the titration curves. IC50 measurements are listed as mean ± standard deviation from 5–8 independent experiments. f Kinase tree illustrating NIK SMI1 kinase selectivity when tested against a panel of 222 kinases. NIK and three potential off-target kinases, KHS1, LRRK2, and PKD1, are marked by colored circles representing percent inhibition observed at 1 μM NIK SMI1
