Table 2.
Selectivity of SS148 and DS0464.
Methyltransferase | IC50 (µM)a | |
---|---|---|
SS148 | DS0464 | |
PRMT1 | 3 ± 0.07 | NI |
PRMT3 | 2 ± 0.07 | NI |
PRMT4 | 1 ± 0.1 | 10 ± 0.8 |
PRMT5 | 9 ± 2 | 13 ± 1.2 |
PRMT6 | 1 ± 0.2 | NI |
PRMT7 | 0.3 ± 0.03 | 14 ± 1.3 |
PRMT8 | 2 ± 0.05 | NI |
PRMT9 | 39 ± 4 | NI |
DOT1L | 0.1 ± 0.009 | 7 ± 0.2 |
DNMT1 | 2 ± 0.3 | NI |
DNMT3A/3L | 0.1 ± 0.002 | NI |
DNMT3B/3L | 0.03 ± 0.006 | NI |
METTL3-METTL14 | 0.9 ± 0.1 | NI |
SETD3 | NI | NI |
BCDIN3D | 0.03 ± 0.002 | 46 ± 9 |
Nsp14 | 0.07 ± 0.006 | 1.1 ± 0.2 |
NI, no inhibition.
IC50 values are presented as the mean ± standard deviation (n = 3).