Figure 2.

CamA inhibition by DOT1L inhibitors. (a) Chemical structures of sinefungin and three DOT1L inhibitors examined. The numerical number in parenthesis refers to our laboratory code. The symbol * in EPZ004777 indicates a substitution of the purine nitrogen with carbon atom. The symbol * in EPZ5676 indicates a chiral atom. (b) Relative inhibition of CamA activity at a single inhibitor concentration of 50 μM. (c) The IC₅₀ measurements were made by varying inhibitor concentrations. The shown codes for the four inhibitors are described in panel A. (d) Isothermal titration calorimetry (ITC) measurement of dissociation constants and stoichiometry (vertical red dash line) of various compounds to CamA. (e) Summary of the IC₅₀ and K_D values of inhibition of methylation of CamA by various inhibitors on DNA substrate.