Figure 5.

Inhibition of full-length WT NSD2 activity toward nucleosomes measured by the radiolabeled HotSpot assay with a 10-point concentration series of inhibitor. DA3003-1 potently inhibits NSD2 with an IC₅₀ value of 0.17 μm (Hill slope = −5.57; n = 4) (A); PF-03882845 inhibits NSD2 activity with an IC₅₀ value of 7.6 μm (Hill slope = −3.68; n = 5) (B); chaetocin is a potent inhibitor of NSD2 activity (IC₅₀ = 0.13 μm; Hill slope = −0.71; n = 5) (C); TC LPA5 4 inhibits NSD2 with an IC₅₀ value of 8.5 μm (Hill slope = −1.5; n = 5) (D); ABT-199 inhibits NSD2 with an IC₅₀ value of 1.7 μm (Hill slope = −1.23; n = 5) (E). The positive control SAH inhibits NSD2 with an IC₅₀ value of 8.2 μm (Hill slope = −0.85; n = 4) (F). Data are plotted as the mean value ± S.D. of n technical replicate experiments.