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Inhibition of 20S proteasome by mono- and bivalent inhibitors (IC50, μM)
| Inhibitor | PGPH | Trypsin-like | Chymotrypsinlike |
|---|---|---|---|
| Ac-LLnL-H (1) | >100 | >100 | 2.1 |
| CO-LLnL-H | |||
| (PEG)x(7) | >100 | >100 | 1.8 |
| COOH | |||
| CO-LLnL-H | |||
| (PEG)x(8) | >100 | >100 | 0.017 |
| CO-LLnL-H | |||
| Ac-RVR-H (2) | >100 | 6.4 | >100 |
| CO-RVR-H | |||
| (PEG)x(9) | >100 | 8.2 | >100 |
| COOH | |||
| CO-RVR-H | |||
| (PEG)x(10) | >100 | 0.071 | >100 |
| CO-RVR-H | |||
| CO-LLnL-H | |||
| (PEG)x(11) | >100 | 0.097 | 0.031 |
| CO-RVR-H |
