Table 1. The inhibitory activity of the compounds against RIP3 and Rafs.
Compounds |
IC50
for RIP3 (μM) |
IC50
for Rafs (nM) |
||||
---|---|---|---|---|---|---|
Luminescent assaysa | Radioactive assaysa | B-Raf | B-RafV600E | C-Raf | Refsb | |
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 | — | — | — |
Abbreviations: NA, not applicable; ND, not determined; RIP, receptor-interacting protein
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
References (refs) reporting the IC50 values of Rafs inhibition by the corresponding compounds
No data reported
No IC50 available at the tested conditions