Table 1 The inhibitory activity of the compounds against RIP3 and Rafs

From: The B-RafV600E inhibitor dabrafenib selectively inhibits RIP3 and alleviates acetaminophen-induced liver injury

Compounds

IC 50 for RIP3 ( μ M)

IC 50 for Rafs (nM)

 

Luminescent assays a

Radioactive assays a

B-Raf

B-Raf V600E

C-Raf

Refs b

Dabrafenib

0.25±0.16

0.002

3.2

0.8

5.0

35

AZ628

0.90±0.15

4.48

100

34

29

36

Regorafenib

2.56±1.02

0.95

28

19

—c

37

PLX4720

4.72±2.25

1.52

—

13

—

38

Vemurafenib

6.73±3.72

14.30

100

31

48

39

Sorafenib

14.52±0.51

NAd

22

—

—

40

GDC-0879

NA

ND

—

0.13

—

41

SB590885

NA

ND

0.16

—

1.72

42

SU11248

NA

ND

—

—

—

 

Necrostatin-1

NA

NA

—

—

—

 
  1. Abbreviations: NA, not applicable; ND, not determined; RIP, receptor-interacting protein
  2. IC50 values from luminescent assays were presented as mean±S.D. from three independent experiments in our laboratory, whereas the IC50 values from radioactive assays were presented as the mean of two independent experiments performed by the Reaction Biology Corporation
  3. bReferences (refs) reporting the IC50 values of Rafs inhibition by the corresponding compounds
  4. cNo data reported
  5. No IC50 available at the tested conditions
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