Table 1.
Overall Inhibition of Caspase-9 Full Length by Peptides
| Peptide | % Inhibitiona (66.7 µM peptide) |
IC50 appb (µM) |
|---|---|---|
| 1 | 0 | >100 |
| 2 | 0 | >100 |
| 3 | 0 | >100 |
| 4 | 1.1± 2.4 | >100 |
| 5 | 0.45 ± 1.1 | >100 |
| 6 | 0 | >100 |
| 7 | 6.3 ± 11 | >100 |
| 8 | 13 ± 16 | >100 |
| 9 | 15 ± 14 | >100 |
| 10 | n.d. | 64 ± 13 |
| 11 | 24 ± 13 | 32 ± 11 |
| 12 | 8 ± 11 | >50 |
| 13 | 0 | >100 |
| 14 | 13 ± 7.1 | 50 ± 3.8 |
| 15 | 0 | >100 |
| 16 | 6.2 ± 2.6 | >100 |
| 17 | 22 ± 23 | 50 ± 5.1 |
| 18 | 17 ± 9.6 | >100 |
| 19 | 24 ± 8.4 | 80 ± 4.8 |
| 20 | 2.2 ± 1.2 | >100 |
| 21 | 2.9 ± 3 | >100 |
| 22 | 0 | >100 |
| 23 | 0 | >100 |
| 24 | 1.8 ± 2.6 | >100 |
| 25 | 2.5 ± 3.5 | >100 |
| 26 | 8.9 ± 12 | >100 |
| 27 | 0 | > 100 |
| 28 | 0 | >100 |
a
Proteolytic cleavage gel-based caspase-9 activity assay which monitors cleavage of natural substrate, caspase-7. Percent inhibition was calculated using Gene Tools (SynGene by producing a standard curve from densiometry values for processed and unprocessed substrate, (caspase-7 C186A).
b
Fluorescence-based caspase-9 activity assays which monitor cleavage of fluorogenic substrate (LEHD-AFC).