Figure 6
From: Discovery of Small Molecules that Inhibit the Disordered Protein, p27Kip1
The small molecule SJ403 displaces p27-D2 from Cdk2/cyclin A and partially restores Cdk2 kinase activity.
Analysis of Cdk2 kinase activity [within the Cdk2/cyclin A complex (200 pM) using Histone H1 as the substrate] in the presence of p27-D2 (200 nM) and varied concentrations of SJ403 (from 10 μM to 3 mM) (a) and varied concentrations of SJ403 alone (b). Cdk2 is partially active under the starting conditions in (a) and activity is enhanced through addition of SJ403. In the absence of p27-D2 (b), addition of SJ403 is associated with Cdk2 inhibition. All experiments were performed in triplicate and average values and the standard deviations of the means are shown.
