Table 6.
Recent examples of lysine methyltransferase inhibitors
| Name | Structure | Potency | KMT specificity | Reference |
|---|---|---|---|---|
| EPZ-6438 |  |
2.5 nM | MT6 | (Knutson et al., 2013) |
| GSK126 |  |
0.5–3 nM | KMT6 | (McCabe et al., 2012) |
| EI1 |  |
9.4 nM | KMT6 | (Qi et al., 2012) |
| BIX-01294 |  |
2.7 µM | KMT1C/D | (Kubicek et al., 2007; Lu et al., 2013) |
| UNC0638 |  |
<15 nM | KMT1C/D | (Vedadi et al., 2011) |
| BRD4770 |  |
6.3 µM | KMT1C/D | (Yuan and Marmorstein, 2012; Yuan et al., 2012) |
| UNC0642 |  |
<2.5 nM | KMT1C/D | (Liu et al., 2013) |
| Bromo-deaza-SAH |  |
77 nM | KMT4 | (Yu et al., 2013) |
| EPZ-5676 |  |
80 pM | KMT4 | (Daigle et al., 2011) |
| SGC0946 |  |
0.3 nM | KMT4 | (Yu et al., 2012) |
| AZ505 |  |
0.12 µM | KMT3C | (Ferguson et al., 2012) |
| Nahuoic acid |  |
2 µM | KMT5A | (Williams et al., 2013) |