Table 1.
Inhibition constants (Ki) for the cGMP-dependent protein kinases. The inhibition constants for kinases PKG-Iα, -Iβ and -II and PKA were determined in vitro.
| Inhibitors | PKG-Iα | PKG-Iβ | PKG-II | PKA-II | Ref. |
|---|---|---|---|---|---|
| Ki (µM) | Ki (µM) | Ki (µM) | Ki (µM) | ||
| (Rp)-cGMP-S | 20 | 15 | 0.5 | 20 | [22,25] |
| (Rp)-8-Br-cGMP-S | 3.7 | 15 | - | 20 | [22] |
| (Rp)-8-Br-PET-cGMP-S | 0.035 | 0.03 | 0.45-0.9 | 11 | [3,10,22,24,35] |
| (Rp)-8-pCPT-cGMP-S | 0.5 | 0.45-0.6 | 0.29-0.7 | 8.3 | [9,10,22] |
| KT-5823 | 0.23 | - | - | > 10 | [23,28] |
| H-7 | 5.8 | - | - | 3 | [1,28] |
| H-8 | 0.5 | - | - | 1.2 | [1,28] |
| H-9 | 0.9 | - | - | 1.9 | [1,28] |
| H-89 | 0.48-0.5 | - | - | 0.05 | [1,23,28] |
| W45 | 0.49-1.15 | - | - | 559 | [2,30] |
| DT-2 | 0.012 | - | - | 12.7-20.3 | [2,30] |
| DT-3 | 0.025 | - | - | 493 | [30] |
| (D)-DT-2 | 0.0008 | - | - | 8.7-15.3 | [34] |
Abbreviation: - not detected.