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. Author manuscript; available in PMC: 2023 Jul 5.
Published in final edited form as: Eur J Med Chem. 2022 Apr 27;237:114407. doi: 10.1016/j.ejmech.2022.114407

Figure 3.

Figure 3.

Mode of inhibition studies for inhibitors of p300 HAT. (A, B) Plots of IC50 values of compound 29 versus increasing concentrations of (A) Ac-CoA (1 - 50 μM, or 0.14 - 7.1× Km) and (B) histone H3 (1-100 μM) suggest the inhibitor is non-competitive against Ac-CoA and competitive against histone; (C) ALPHA assay results show inhibitors 29 and 3 can dose-dependently disrupt the binding between p300 HAT and histone H4, while such binding was not significantly inhibited by inactive compound 6 as well as A-485 (an Ac-CoA competitive inhibitor).