表2 ONX-0914及衍生物的蛋白酶体抑制活性及选择性 [ 12, 18]
Table 2 Proteasome inhibitory activities and selectivities of ONX-0914 and its derivatives [ 12, 18] (nmol/L)
|
化合物 |
蛋白酶体抑制活性(IC 50) |
选择性(β5c/β5i) |
|||||
|
β1i |
β1c |
β2i |
β2c |
β5i |
β5c |
||
|
ONX-0914 |
460 |
>10 4 |
590 |
1100 |
5.7 |
54 |
9 |
|
PR-924 |
1840 |
>10 4 |
>10 4 |
>10 4 |
2.5 |
227 |
91 |
|
LU-005i |
300 |
>10 4 |
410 |
2500 |
6.6 |
287 |
43 |
|
LU-025i |
>10 4 |
>10 4 |
>10 4 |
>10 4 |
36 |
1900 |
53 |
|
LU-045i |
>10 4 |
>10 4 |
>10 4 |
>10 4 |
32 |
827 |
26 |
|
LU-015i |
7100 |
>10 4 |
>10 4 |
>10 4 |
8.3 |
4600 |
553 |