TABLE 2.
Effects of RM-1-132 on WT and mutant CDPK1 and parasites
| Cell line (CDPK1) | EC50 shifta (μM) | IC50 (μM) | TSA |
TSA + EGTA |
L-CETSAc |
IC-CETSAc |
||||
|---|---|---|---|---|---|---|---|---|---|---|
| Tm (°C) | Thermal shift (°C) | Tm (°C) | Thermal shift (°C) | Tm (°C) | Thermal shift (°C) | Tm (°C) | Thermal shift (°C) | |||
| RH (WT) | NA | 0.003 | 50.7 ± 0.9b | 12.3 ± 0.5 | 54.8 | 11.3 | 48.0 | 12.2 | 50.9 | 6.0 |
| A-f8 (H201Q) | 4.1 | 0.002 | 47.8 ± 0.6 | 11.4 ± 0.5 | 51.0 | 11.2 | 49.4 | 9.0 | 50.1 | 3.0 |
| C-d12 (L96P) | 9.7 | 0.004 | 43.4 ± 0.8 | 9.2 ± 0.5 | 48.1 | 9.2 | 49.9 | 6.0 | 48.5 | 2.7 |
a
EC50 fold shift compared to that for the RH parental strain. NA, not applicable.
b
The standard deviation is provided when at least three separate assays were done.
c
Data points for the cell lysate and intact cell assays are shown in Fig. 5B.