Table 1. HGFA, Matriptase and Hepsin Inhibitory Activity of Pro-HGF and Pro-MSP Substrate-Based Inhibitors.
| structure | HGFA Ki (nM) | matriptase Ki (nM) | hepsin Ki (nM) |
|---|---|---|---|
| nafamostat | 25 | 0.02 | 0.53 |
| leupeptin (Ac-LLR-H) | 188 | 696 | 61 |
| Ac-KQLR-kt(pro-HGF; 5) | 53 | 0.92 | 0.22 |
| Ac–KHLR-kt (5a) | 96 | 22 | 0.41 |
| Ac-WQLR-kt (5b) | 65 | 32 | 0.21 |
| Ac-KQFR-kt (5c) | 58 | 0.69 | 0.58 |
| Ac–KFLR-kt (5d) | 80 | 15 | 2.1 |
| Ac-RQLR-kt (5e) | 60 | 0.32 | 0.28 |
| Ac-SQLR-kt (5f) | 182 | 9.2 | 0.34 |
| Ac–KRLR-kt (5g) | 12 | 1.1 | 0.57 |
| Ac-WRLR-kt (5h) | 21 | 5.5 | 0.21 |
| Ac-SKLR-kt(pro-MSP; 6) | 81 | 58 | 1.2 |
| Ac–SHLR-kt (6a) | 332 | 104 | 0.60 |
| Ac-WKLR-kt (6b) | 56 | 8.6 | 0.55 |
| Ac-SKFR-kt (6c) | 57 | 3.0 | 8.5 |
| Ac-NKLR-kt (6d) | 79 | 12 | 1.4 |
| Ac–SRLR-kt (6e) | 24 | 5.8 | 0.68 |
| Ac-TKLR-kt (6f) | 103 | 8.7 | 0.61 |
| Ac–SWLR-kt (6g) | 63 | 69 | 1.2 |
| Ac-RKLR-kt (6h) | 17 | 0.83 | 0.47 |