TABLE 1.

DNMT1 and DNMT3Acat inhibition activity of SGI-1027 and its analogs and differences in the T_m values of the duplexes in the presence and in the absence of the compounds (ΔT_m)

The concentrations (μm) at which 50% of the methylation activity is inhibited (IC₅₀) are reported for DNMT3Acat and DNMT1. For 19, the percentages of inhibition are displayed. The difference in T_m (ΔT_m in °C) in the presence of 10 μm of inhibitors and in their absence is reported for each duplex. Means of at least two experiments with the corresponding standard errors are reported. The means of measured T_m are displayed in parentheses (°C).

Compounds	IC50		ΔTm (measured Tm in °C) at 10 μm
	DNMT3Acat	DNMT1	hp_2_CG	hp_1_CG	hp_0_CG
	μm		°C
SGI-1027	0.8 μm ± 0.1 μm	10 μm ± 1 μm	−0.5 ± 0.0 (74.0)	1.0 ± 0.0 (72.0)	0.5 ± 0.0 (68.5)
5	0.7 μm ± 0.5 μm	5.7 μm ± 0.2 μm	1.5 ± 0.0 (76.0)	3.0 ± 0.0 (74.0)	4.0 ± 0.0 (72.0)
31	0.9 μm ± 0.2 μm	15 μm ± 3 μm	0.3 ± 0.3 (74.8)	1.1 ± 0.2 (72.1)	1.6 ± 0.4 (69.6)
19	<10% of inhibition at 10 μm	<10% of inhibition at 10 μm	0.5 ± 0.0 (75.0)	0.5 ± 0.0 (71.5)	0.3 ± 0.3 (68.3)