Table 1. Comparison of the inhibition activity of various PARP inhibitors between PARP1 and bacterially expressed GST-TIPARP.
Inhibitor | IC50 (M) | |
---|---|---|
PARP1 | TIPARP | |
3ABA | 1.7 ± 0.4 × 10−4* | 9.8 ± 4.0 × 10−4 |
PJ34 | 5.5 ± 1.4 × 10−8* | 2.6 ± 1.1 × 10−5 |
Olaparib | 1.4 ± 0.04 × 10−7* | 8.0 ± 2.0 × 10−7 |
KU0058948 | 7.6 ± 0.4 × 10−8 | n.d. |
Abbreviations: n.d., not determined because greater than 50% inhibition was not achieved.
Significantly different compared with treatment matched TIPARP.