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. Author manuscript; available in PMC: 2014 Jun 5.
Published in final edited form as: Cancer Cell. 2011 Jul 12;20(1):53–65. doi: 10.1016/j.ccr.2011.06.009

Figure 1. Biochemical Characterization of EPZ004777 Inhibition of DOT1L.

Figure 1

(A) Chemical structure of EPZ004777.

(B) Inhibition of recombinant human DOT1L by EPZ004777. Each data point represents the mean of two replicates at each specified concentration of compound. The data are fit to a standard Langmuir isotherm equation for inhibition (Copeland, 2005).

(C) Plot of IC50 values of EPZ004777 as a function of SAM concentration relative to the Km of S-adenosylmethionine (SAM) ([SAM]/Km). These values display a linear relationship as expected for SAM-competitive inhibition with a Ki of 0.3 ± 0.03 nM (± error represents standard error of the mean [SEM]).

(D) Plot of IC50 values for EPZ004777 against a panel of human HMT enzymes.