TABLE 1.
Active sites |
IC50 ratio |
||||
---|---|---|---|---|---|
β5i | β2i | β1i | β2i/β5i | β1i/β5i | |
IC50 (μm) | -fold | ||||
NC-005 | 0.044 | 4.6 | 10 | 105 | 225 |
NC-005-mvs | 1.5 | ∼140 | ∼140 | ∼93 | ∼93 |
YU-101 | 0.26 | 1.9 | 4.5 | 7.3 | 17.3 |
YU-101-mvs | 1.9 | ≫100a | ≫100b | ||
PR-171 | 0.00028 | 0.62 | 2.42 | 2321 | 8643 |
PR-171-mvs | 0.011 | 5.3 | 22.5 | 481 | 2045 |
PR-957 | 0.0102 | 1.04 | 6.4 | 102 | 627 |
PR-957-mvs | 1.0 | 53 | 78 | 53 | 78 |
a 21 ± 1% inhibition was at 81 μm.
b 16 ± 2% inhibition was at 81 μm (values are mean ± S.E. of two independent measurements).