Table 1.

Enzymatic characterization of wild-type SETD7 and mutants

ProteinKmapp, µMkcat, h−1(R)-PFI-2 IC50, nM*
PeptideSAM
Wild-type1.1 ± 0.10.3 ± 0.148 ± 22.0 ± 0.2
H252W1.8 ± 0.20.5 ± 0.137 ± 42,630 ± 200
D256A1.9 ± 0.10.4 ± 0.17 ± 11,200 ± 90
V274E3.1 ± 0.20.7 ± 0.23 ± 0.510,770 ± 2,000
  • * Methods are described in SI Appendix. All experiments were performed in triplicate, and values are presented as mean values ± SD.