Table 1.
Determination of kcat values in the presence of the active compounds using peptide or nucleosome as substrate.
Compound | kcat (h−1) | |||
---|---|---|---|---|
H3(21–44) | Human nucleosome | |||
PRC2-WT | PRC2-EED-I363M | PRC2-WT | PRC2-EED-I363M | |
DMSO (control) | 24 ± 1 | 9 ± 1 | 2.5 ± 0.06 | 0.7 ± 0.04 |
1 (UNC5635) | 25 ± 0.5 | 20 ± 1 | 1.7 ± 0.05 | 1.3 ± 0.01 |
2 (UNC5636) | 24 ± 0.5 | 21 ± 1 | 1.6 ± 0.04 | 1.5 ± 0.02 |
4 (UNC6008) | 20 ± 1 | 12 ± 0.5 | 1.1 ± 0.04 | 0.8 ± 0.02 |
Data shown are mean ± SD, n = 3.