Table 1 Caspase inhibition activity of P2-stereospecific LJ2a, LJ2b, LJ3a, and LJ3b compounds against Casp-2 vs. Casp-3.
From: Genuine selective caspase-2 inhibition with new irreversible small peptidomimetics
Casp2 | Casp3 | |||||
|---|---|---|---|---|---|---|
Compounds | k3 | Ki | k3/Ki | k3 | Ki | k3/Ki |
(ms−1) | (nM) | (M−1 s−1) | (ms−1) | (nM) | (M−1 s−1) | |
LJ2a | 5 ± 5 × 10−4 | 0.9 ± 0.1 | 5,499,419 | 1.3 ± 4 × 10−5 | 11.5 ± 0.9 | 113,425 |
LJ2b | 4 ± 3 × 10−4 | 524 ± 10 | 7177 | 8 ± 2 × 10−3 | 17,498 ± 104 | 457 |
LJ3a | 5 ± 7 × 10−4 | 2.8 ± 0.8 | 1,708,996 | 0.7 ± 9 × 10−5 | 399.8 ± 93.3 | 1807 |
LJ3b | 7 ± 10−3 | 8539 ± 300 | 823 | 0.8 ± 6 × 10−5 | 84,205 ± 1300 | 9 |
