Figure 3.

Models of slow-binding inhibition and continuous inhibition of HDACs 1–3 by compound 3. (A) Mechanisms A and B of competitive slow-binding inhibition and calculation of inhibitor constants (K_i) from kinetic data. (B) Continuous assay progression curves for the inhibition of HDACs 1–3 by different concentrations of 3. (C) Secondary plots of the apparent first-order rate constant for equilibration (k_obs) vs inhibitor concentration and fits to mechanism B of slow-binding kinetics (see Table 1 for numerical data). Data represent mean ± SEM of individual experiments, with each experiment performed at least twice. *The HDAC3 preparation contained the DAD of NCoR2.