Table 1 IC50 values obtained for each β-subunit
Proteasome subunit | AMO-1 | AMO-BTZ | AMO-CFZ | |
---|---|---|---|---|
BTZ | ||||
IC50 (nm) (50% functional proteasome inhibition) | β2c | NA | NA | NA |
β2i | NA | NA | NA | |
β1c | 40 | 60 | 50–60 | |
β1i | 20–25 | 50 | 50–60 | |
β5c | 25 | 80–90 | 50–60 | |
β5i | 30 | 80–90 | 50–60 | |
LD50 (nm) (50% cell viability) | 50 | >1000 | >1000 | |
CFZ | ||||
IC50 (nm) (50% functional proteasome inhibition) | β2c | 300 | 220 | >1000 |
β2i | 180 | 90 | 800 | |
β1c | >500 | 600 | >1000 | |
β1i | >250 | 250 | 1000 | |
β5c | 10 | 50 | 90 | |
β5i | 10 | 50 | 250 | |
LD50 (nm) (50% cell viability) | 150 | >1000 | >1000 |