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Examples of oxamyl dipeptide caspases inhibitors with various leaving groups.299
|
enzyme assays k3/Ki, M−1s−1 | cellular assays IC50, μM | - | ||||
|---|---|---|---|---|---|---|---|
| mCasp-1 | Casp-3 | Casp-6 | Casp-8 | JFas | THP-1 | a-Fas liver, IP, ED50 mg.kg | |
| -O(2,3,5,6-F4-Ph) 243 IDN-6556 |
689000 | 75700 | 58700 | 2940000 | 0.025 | 0.27 | 0.08 |
| -OPOPh2 271 | 2158000 | 99100 | 52100 | 2010000 | 0.081 | 9.09 | 0.14 |
| -OCO(2,6-Cl2-Ph) 272 | 8330000 | 236000 | 105000 | 4300 | 0.143 | 11.8 | 45.8 |
