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. 2015 Feb 9;6(5):2782–2789. doi: 10.1039/c4sc03739a

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.