TABLE 1

Ki values for VRT-043198 against caspases and noncaspase proteases


Caspases

Noncaspase Proteases
Enzyme
Ki
Enzyme
Ki
nM nM
Caspase-1 (ICE) 0.8 Granzyme B 9000
Caspase-4 <0.6 Cathepsin B 48% inhibition at 100 μM
Caspase-8 100 Trypsin 4% inhibition at 100 μM
Caspase-6 560
Caspase-9 1030
Caspase-7 16,000
Caspase-3
21,500