Table 2. IC50 values for EI1, EPZ-6438 and compound 3 against PRC2WT, PRC2Y111L, PRC2Y641N and PRC2Y641N/Y661D.
| Inhibitor | Substrate | WT (μM) | Y111L (μM) | Y641N (μM) | Y641N/Y6661D (μM) |
|---|---|---|---|---|---|
| EI1 | Me0 | 0.2±0.03 | >25 | (−) | (−) |
| Me1 | 0.06±0.0 | >25 | 0.1±0.03 | >25 | |
| Me2 | (−) | (−) | 0.2±0.05 | >25 | |
| EPZ-6438 | Me0 | 0.2±0.04 | 11.5±4.3 | (−) | (−) |
| Me1 | 0.06±0.01 | 9.2±2.7 | 0.1±0.03 | 2.8±1.1 | |
| Me2 | (−) | (−) | 0.1±0.04 | 3.4±0.8 | |
| Compound 3 | Me0 | 2.02±0.4 | >25 | (−) | (−) |
| Me1 | 0.9±0.2 | >25 | 6.1±0.8 | >25 | |
| Me2 | (−) | (−) | 8.7±1.1 | >25 |
Abbreviation: WT, wild type.
The biochemical reaction was carried out with [SAM] at 20 μM. The assay was carried out with [SAM] of 20 μM. When indicated with (-), those conditions were not tested due to low basal activity.