Table 1.
Kinetic equilibrium dissociation constant (KD) values for binding of Spongionella derived compounds and CsA to CypA.
| KD (nM) | Calcineurin inhibition (%) | IL-2 release (%) | |
|---|---|---|---|
| Gracilin L | 24.85 ± 6.83 | ≈ 10 | 71.8 ± 11.6 |
| Compound 1 | 5.34 ± 1.68 | 22.3 ± 6.1 | 44.5 ± 2.15 |
| Compound 2 | 7.67 ± 1.61 | 31.0 ± 3.4 | 36.1 ± 5.9 |
| Cyclosporin A | 6.83 ± 1.1 | 17.3 ± 4.5 | 66.75 ± 8.25 |
Inhibition of calcineurin phosphatase activity expressed in percentage of control cells. IL-2 inhibition is expressed in the percentage of control cells. For calcineurin and IL-2 experiments, cells were treated with GraL (1 μM), compounds 1, 2 (0.1 µM), or CsA (0.2 µM) for 2 h and then were stimulated with Con A (50 μg/mL) for 48 h.