Table 3.
Structure and inhibition data of S10 and C13 analogues.
| Compound | Structure | % Inhibition with 100 µM compound | IC50 (µM)* |
|---|---|---|---|
| S10G |
|
98.6 ± 2.4a 99.1 ± 1.5c |
4.2 ± 0.3 |
| S10L |
|
89.0 ± 3.0a 90.5 ± 5.2c |
4.4 ± 0.4 |
| S10K |
|
81.7 ± 2.0a 81.7 ± 3.4c |
7.6 ± 0.8 |
| S10D |
|
96.3 ± 1.6a 53.3 ± 7.8b |
9.8 ± 1.7 |
| S10B |
|
92.0 ± 6.7a 64.4 ± 14.7b |
10.5 ± 2.4 |
| S10C |
|
96.8 ± 0.7a 62.9 ± 6.8b |
11.0 ± 1.3 |
| S10E |
|
94.6 ± 1.1a 46.8 ± 7.4b |
12.8 ± 1.8 |
| S10F |
|
93.7 ± 0.8a 52.5 ± 6.5b |
12.9 ± 1.3 |
| S10M |
|
81.3 ± 3.3a 43.7 ± 3.1b |
16.4 ± 3.1 |
| S10H |
|
92.3 ± 2.7a 53.4 ± 10.4b |
16.5 ± 2.3 |
| S10I |
|
74.3 ± 5.8a 81.8 ± 4.6c |
16.8 ± 2.2 |
| S10P |
|
59.3 ± 2.5a 44.7 ± 4.7b |
79.9 ± 9.9 |
| C13G |
|
55.5 ± 8.8a | 21.5 ± 2.0 |
| C13F |
|
43.2 ± 10.9a | 27.0 ± 1.6 |
| C13C |
|
24.7 ± 1.7a | 719 ± 76** |
| C13A |
|
21.8 ± 2.5a | 1545 ± 261** |
| C13B |
|
2.3 ± 3.1a | 1922 ± 300** |
| C13D |
|
5.5 ± 4.1a | 2047 ± 57** |
| C13E |
|
−8.3 ± 1.7a | 3370 ± 678** |
aFluorescence assay, bcolorimetric assay, cCasp6-C163A cleavage assay, *IC50 values were determined using fluorescence assay, **approximate IC50 values calculated from not-perfectly fitted dose-response curves due to limited compound solubility (C13A, C13C) or very low compound potency at the highest concentration tested (C13B, C13D, C13E).