Table 1

In vitro potencies of SK inhibitors against various kinases

Potencies of each inhibitor were determined for human isoforms of ERK2, PI3k, and PKC-α. GST-hSK inhibition data is provided for comparison. Data represent the concentrations required to inhibit enzyme activity by 50% and are the mean ± SD of triplicate experiments. None: no inhibition detected up to 60 μm.

CompoundGST-hSKhERK2hPI3khPKCα
I1.2 ± 0.311 ± 1NoneNone
II0.5 ± 0.3NoneNoneNone
III2.5 ± 0.726 ± 242 ± 10None
IV0.6 ± 0.140 ± 57 ± 2None
V2.0 ± 0.280 ± 46 ± 2None