Figure 3.
(a) Pilot screen of p300 and Gcn5 using an epigenetic-targeted inhibitor library. Percent activity represents relative KAT-catalyzed turnover of FITC-peptide in the presence of compound compared to vehicle DMSO control. All reactions were quenched and analyzed under conditions where enzyme velocity was linear. (b) Structures of selected compounds which showed >40% inhibition of p300 or Gcn5 at 40 μM. Color code for highlighted compounds: yellow, p300 inhibitors; green, Gcn5 inhibitors; orange, inhibitor of both p300 and Gcn5.
