Table 28.
enzyme assays IC50, μM | |||||||
---|---|---|---|---|---|---|---|
mCasp-1 | Casp-3 | Casp-6 | Casp-7 | Casp-8 | Ref | ||
Ac-DEVD-CHO | 83 | 0.05 | 0.0035 | 0.01 | 0.01 | 0.08 | 275 |
1-Naphthyloxy acetyl | 277 | 0.570 | 0.135 | 0.940 | 1.81 | 0.770 | |
2- Naphthyloxy acetyl | 278 | 10 | 0.944 | 18.56 | 8.87 | > 10 | |
2-(1-Naphthyloxy)propionyl | 279 | 3.99 | 0.376 | 1.28 | 1.32 | 2.43 | |
1-Naphthylmercapto acetyl | 280 | 2.75 | 0.195 | 1.43 | 1.74 | 7.42 | |
3-(1-Naphthyloxy)propionyl | 281 | 0.686 | 0.059 | 0.305 | 1.37 | 9.81 | |
4-Methoxy-1-naphthyloxy acetyl | 282 | 0.831 | 0.263 | 22.6 | 4.08 | 1.45 | |
4-Chloro-1-naphthyloxy acetyl | 283 | 0.429 | 0.231 | 12.0 | 3.38 | 1.69 | |
2,4-Dichloro-1-naphthyloxy acetyl | 284 | 0.141 | 0.357 | 21.4 | 3.61 | 3.04 | |
2-Biphenoxy acetyl | 285 | 0.636 | 0.095 | 0.717 | 2.02 | 1.71 | |
(2-Cyclopentyl)phenoxy acetyl | 286 | 0.538 | 0.197 | 3.37 | 1.49 | 1.86 | |
| |||||||
enzyme assays IC50, μM | Cell assay IC50, μM | ||||||
Casp-1 | Casp-3 | Casp-7 | Casp-8 | NT2 cells | Ref | ||
| |||||||
Ac-DEVD-CHO | 83 | 0.19 | 0.027 | 0.087 | 0.13 | > 100 | 306 |
2,5-di-(OCH3)-Ph-CH2- | 287 | 6.0 | 0.048 | 3.2 | 6.6 | 10 | |
2,4-di-Br-Ph-CH2- | 288 | 0.86 | 0.14 | 1.5 | 8.7 | 63.0 | |
5-fluoro-1H-indole- | 289 | 2.6 | 0.083 | 1.4 | 3.3 | 55.0 | |
2-CH3O-Ph-CH2- | 290 | 28 | 0.31 | 2.7 | 15.5 | - | |
3-CH3O-Ph-CH2- | 291 | 14 | 0.21 | 3.1 | 14 | 60.0 | |
Ph-CH2- | 292 | 22 | 0.75 | 8.4 | 22.5 | - | |
2-CH3O-4-Br-Ph-CH2- | 293 | 3.1 | 0.06 | 3.1 | 2.3 | 9.0 | |
2-CH3O-4-acetyl-Ph-CH2- | 294 | 5.9 | 0.01 | 0.13 | 2.9 | 2.0 |