A conjugate comprising a pyrrole-imidazole polyamide that recognizes a specific DNA sequence and a bromodomain inhibitor, a composition for regulating biochemical activity, specifically for regulating histone modification, e.g., for inducing histone acetylation, which comprises the conjugate, a composition for recruiting a bromodomain-containing protein which comprises the conjugate, a method for nucleosome acetylation which comprises using the conjugate, and a method for bromodomain-containing protein recruitment which comprises using the conjugate are provided.