Table 1. In vitro and in situ inhibition of recombinant human GH29 α-l-fucosidase, given as half-maximal inhibitory concentration (IC50) a .
In vitro IC50 | In situ IC50 | |
Aziridine | ||
1 (JJB256) | 6.9 ± 0.8 | 28.9 ± 4.4 |
2 (JJB244) | 8.7 ± 1.2 | 157.8 ± 22 |
3 (JJB243) | 7.2 ± 1.1 | 25 512 ± 2278 |
4 | 371.6 ± 21.2 | 515.4 ± 72.9 |
5 | 46.8 ± 3.4 | 77.9 ± 9.1 |
23 | 8.7 ± 1.1 | 65.4 ± 7.5 |
Iminosugars | ||
6 | 3979 ± 257 | ND |
7–13 | >100 000 | ND |
aValues are given in nanomolar. ND: not determined. It should be noted that IC50 values on competitive inhibitors do not compare well to those obtained for mechanism-based inhibitors. The values given above allow for a comparison of inhibitory potency within the two classes of compounds studied.