TABLE 1.
Interaction of BKIs with CDPK1
| Compounda | IC50 (μM)b | EC50 (μM)c | Thermal shiftd (°C) by: |
||
|---|---|---|---|---|---|
| TSA | L-CETSA | IC-CETSA | |||
| 1265 | 0.004 | >6.25 | 7.4 | 6.6 | 0.7 |
| 1294 | 0.003 | 0.14 | 11.9 | 10.9 | 5.0 |
| 1553 | 0.001 | 0.06 | 12.0 | 10.1 | 3.3 |
| 1568 | 0.001 | 0.76 | 11.3 | 5.9 | 0.8 |
| RM-1-132 | 0.003 | 0.09 | 12.3 | 12.1 | 6.0 |
a
The EC50s and IC50s of compounds 1265, 1294, and RM-1-132 (12) and of compound 1553 (9) were published previously. The RM-1-132 EC50 shown here includes additional data from the current work.
b
The assay likely does not discriminate between IC50s of 1 nM or less.
c
EC50 in a 48-h invasion/growth assay.
d
Shifts in the measured Tm compared to that for the solvent (DMSO) control. CDPK1 Tms were as follows: for purified recombinant protein (no EGTA), 50.7 ± 0.9°C; for lysate, 48.0 ± 0.5°C; and for intact cells, 50.1 ± 1°C.