Table 1.
IC50 (μM) ** | SIapp | SIapp | ||||
---|---|---|---|---|---|---|
|
||||||
Mtb20SOG (LLVY) | c-20S β5c (LLVY) | i-20S β5i (ANW) |
|
|
||
DPLG-2 * | 0.015 | 70.00 | 54.70 | 4667 | 3647 | |
PKS2169 | 0.041 ± 0.006 | 29.2 ± 6.6 | 3.75 ± 0.60 | 712 | 91 | |
PKS2144 | 0.010 ± 0.002 | 0.657 ± 0.087 | 0.007 ± 0.001 | 65.7 | 0.7 | |
PKS2205 | 0.023 ± 0.002 | 20.95 ± 6.92 | 2.64 ± 0.62 | 911 | 115 | |
PKS2206 | 0.016 ± 0.001 | 2.57 ± 0.75 | 0.044 ± 0.020 | 161 | 2.8 | |
PKS2208 | 0.016 ± 0.002 | 14.34 ± 3.81 | 0.512 ± 0.157 | 896 | 32 | |
MG-132 | 1.714 ± 0.079 | 0.008 ± 0.001 | 0.024 ± 0.001 | 0.005 | 0.014 |
Data from 20.
Data are given as mean ± SEM.
ANW: Ac-ANW-AMC
LLVY: suc-LLVY-AMC
SIapp: apparent selectivity index