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Organic and Medicinal Chemistry Letters
Figure 3 | Organic and Medicinal Chemistry Letters

Figure 3

From: Discovery of indole tetrafluorophenoxymethylketone-based potent novel small molecule inhibitors of caspase-3

Figure 3

Time-dependent inhibition of caspase-3 activity with NCEs. Caspase-3 at a 20× concentration, as specified in the ‘Methods’ section, was pre-incubated with 20× NCE (the final compound concentration is approximately tenfold higher than respective IC50s). The mixture was pre-incubated for 30 and 60 min at 30°C and then diluted 100-folds with assay buffer containing 10-μM AC-DEVD-AMC. The enzyme activity was measured at 30°C after 30 min. As a control, a mixture of 1× caspase-3 and 1× NCE was prepared and incubated for the same time duration before addition of the substrate. The percentage inhibition was calculated relative to the activity of caspase-3, which went through all the procedures for concentrated or control samples but without the inhibitor. Note that compounds 1A to 3E are from indole, and 4A to 4F from oxalamide series.

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