Table 1.
APO | 2-PCPAa | MS275b | InsP6c | |
---|---|---|---|---|
Post-equilibrium Apparent Parameters | ||||
kcat,post (s−1) | 0.032 ± 0.002 | 0.0077 ± 0.0012 | 0.023 ± 0.003 | 0.093 ± 0.007 |
KM,post (μM) | 2.3 ± 1.7 | 26 ± 5 | 9.2 ± 1.6 | 190 ± 30 |
kcat,post/KM,post (s−1mM−1) | 14 ± 7 | 0.30 ± 0.02 | 2.5 ± 0.4 | 0.48 ± 0.04 |
Unimolecular Exchange | ||||
Keq(E) | 7.0 ± 2.4 | 7.4 ± 0.5 | 1.7 ± 0.6 | 3.0 ± 0.3 |
kex(E) (s−1) | 0.0074 ± 0.0024 | <5 × 10−4 | 0.0028 ± 0.0015 | 0.0015 ± 0.0013 |
Keq(ES) | 76 ± 28 | 129 ± 30 | 146 ± 38 | 49 ± 4 |
kex(ES) (s−1) | 0.0055 ± 0.0012 | 0.0050 ± 0.0008 | 0.0060 ± 0.0024 | 0.047 ± 0.020 |
The 200 nM CoREST complex was pre-equilibrated with 0.1 mM 2-PCPA LSD1 inhibitor.
The CoREST complex was pre-equilibrated with 5 μM MS275 HDAC inhibitor.
The CoREST complex was pre-equilibrated with 0.1 mM InsP6.