Table 1.
Compound |
kassociation = kobs/[I] (M−1s−1)
|
||
---|---|---|---|
Chymotrypsin-like activity | Trypsin-like activity | PGPH activity | |
Epoxomicin | 35,400 ± 1400 | 287 ± 71 | 34 ± 4.8 |
(40–80 nM) | (6–10 μM) | (25–75 μM) | |
clasto-lactacystin | 8,530 ± 280 | 253 ± 41 | 37 ± 4.7 |
β-Lactone | (200–400 nM) | (6–10 μM) | (25–75 μM) |
NLVS | 6,790 ± 919 | 5.3 ± 2.8 | 6.4 ± 2.3 |
(200–400 nM) | (50–100 μM) | (50–100 μM) |
The rate of covalent inhibition (kassociation) of the three major proteasome catalytic activities were determined for epoxomicin, clasto-lactacystin β-lactone, and peptide vinyl sulfone, NLVS. A range of concentrations was used to determine the kassociation for inhibition of individual enzymatic activities.