Table 3.
Inhibition of VIM-2 and VIM-24 by BTZsa
compound | VIM-2
|
VIM-24
|
||||||
---|---|---|---|---|---|---|---|---|
Ki (μM) | Ki* (μM) | k2 (s−1) | k−2 (s−1) | Ki (μM) | Ki* (μM) | k2 (s−1) | k−2 (s−1) | |
L-CS319 | 3.7 ± 0.3 | 0.04 ± 0.01 | (0.03 ± 1) × 10−3 | (0.0003 ± 1) × 10−4 | 6.0 ± 0.7 | 0.12 ± 0.02 | (0.06 ± 2) × 10−3 | (0.001 ± 1) × 10−3 |
D-CS319 | 5.4 ± 0.4 | 0.18 ± 0.02 | (0.01 ± 1) × 10−3 | (0.0003 ± 1) × 10−4 | 11 ± 0.8 | 0.64 ± 0.01 | (0.07 ± 4) × 10−3 | (0.004 ± 1) × 10−3 |
L-VC26 | 3.8 ± 0.2 | 0.25 ± 0.01 | (0.02 ± 1) × 10−3 | (0.001 ± 1) × 10−3 | 4.9 ± 0.3 | 0.13 ± 0.02 | (0.04 ± 2) × 10−3 | (0.001 ± 1) × 10−3 |
D-VC26 | 14 ± 1 | 0.10 ± 0.03 | (0.09 ± 4) × 10−3 | (0.0006 ± 4) × 10−4 | 12 ± 3 | 0.08 ± 0.01 | (0.01 ± 3) × 10−3 | (0.00007 ± 1) × 10−5 |
Ki determined from the initial rate of hydrolysis (v0). Ki* and k2 were calculated from the analysis of the change in vs with inhibitor concentration, in the slow binding model.