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Inhibition of prototypic cyclophilins by compounds 1 and 2
| Enzyme | KI (μM) | |
|---|---|---|
| 1 | 2 | |
| CypA | 0.52 ± 0.15 | 0.3 ± 0.1 |
| CypB | >100 | 12 ± 5 |
| CypC | >100 | >100 |
| PPIL1 | 29 ± 7 | >100 |
| CypD | 2.42 ± 0.76 | 6.28 ± 0.73 |
| USA-Cyp | >100 | >100 |
KI values were determined with the protease-free PPIase assay according to Janowski et al. (46) in 35 mM HEPES buffer pH 7.8 at 283 K, using Suc-Ala-Ala-Pro-Phe-pNA (60 μM) as substrate and increasing concentrations of aryl 1-indanylketones, respectively.
