Table 3.
Compound biological activity and efficacy information.
| Inhibitor | Target IC50 (μM) | Test conc. (μM) | Cmax free (μM) | Reference | |||
|---|---|---|---|---|---|---|---|
| PI3KIs | p110α | p110β | p110δ | p110γ | |||
| NVP-BEZ235 (Dactolisib) | 0.004 | 0.075 | 0.007 | 0.005 | 0.03 - 0.3 - 3 - 30 | 0.02 | IC50: (23–25) Cmax: (26) |
| LY 294002 | 0.5 | 0.973 | 0.57 | 0.3 - 3 - 30 - 300 | (27) | ||
| GDC-0941 (Pictilisib) | 0.003 | 0.033 | 0.003 | 0.075 | 0.03 - 0.1 - 0.3 - 1 | 0.1 | IC50: (28) Cmax: (29, 30) |
| HS-173 | 0.0008 | 0.03 - 0.1 - 0.3 - 1 | IC50: (31) | ||||
| TGX-221 | 0.005 | 0.1 - 0.3 - 1 - 3 | IC50: (32) | ||||
| CAL-101 (Idelalisib) | 0.82 | 0.056 | 0.0025 | 0.089 | 0.2 - 2 - 20 - 200 | 0.7 | IC50: (33) Cmax: (34) |
| CZC24832 | 1.1 | 0.027 | 0.01 - 0.1 - 1 - 10 | IC50: (35) | |||
| ROCKs | ROCK1 | ROCK2 | |||||
| RKI-1447 | 0.0145 | 0.0062 | 0.1 - 0.3 - 1 - 3 | IC50: (36) | |||
| Fasudil | 0.465 | 0.509 | 0.3 - 3 - 30 - 300 | IC50: (37, 38) | |||
| Y-27632 | 0.093 | 0.089 | 0.3 - 3 - 30 - 300 | IC50: (39–43) | |||
| GSK-429286 | 0.014 | 0.063 | 0.03 - 0.3 - 3 - 30 | IC50: (44, 45) | |||
| GSK-3s | GSK-3α | GSK-3β | |||||
| CHIR99021 | 0.01 | 0.0067 | 0.03 - 0.1 - 0.3 - 1 | IC50: (46) | |||
| SB 216763 | 0.034 | 0.03 - 0.1 - 0.3 - 1 | IC50: (47) | ||||
| TWS119 | 0.03 | 0.03 - 0.1 - 0.3 - 1 | IC50: (48) | ||||
The lowest in vitro test concentration with functionally relevant (>20%) reduction in hSC-CMs indices is indicated by the bold format.