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. 2019 Dec 25;48(6):688–694. [Article in Chinese] doi: 10.3785/j.issn.1008-9292.2019.12.15

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