FIGURE 6.

Thermal shifts analysis of SGI-1027 and its analogs in complex with human DNMT1. A, effect of 5, 19, 31, and SGI-1027 incubated at 200 μm with 2.5 μm DNMT1 alone (white bars) or in the presence of 5 μm AdoMet and of DNA (black bars). B, effect of the AdoMet and DNA substrates. For each condition, DNMT1 was incubated at 2.5 μm with 200 μm compound 5, and 5 μm AdoMet and/or 5 μm DNA duplex. C, concentration effect of 5 (5–200 μm). DNMT1 alone at 2.5 μm (white bars) or in the presence of 5 μm AdoMet and DNA (black bars) was incubated with increasing concentrations of compound 5. D, effect of increasing concentrations of AdoMet (from 2.5 to 25 μm) on 2.5 μm DNMT1 alone (white bars) and in the presence of 5 μm DNA (black bars) incubated with 200 μm SGI-1027. The means of at least two experiments are displayed with the corresponding S.E.