Table 2.
In Vitro Potencies of PARP Inhibitorsa
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Veliparib | Niraparib | Olaparib | Talazoparib | Rucaparib | PJ34 | 1 (UPF1069) | |||||||||
Protein | Construct | pIC50 | IC50 | pIC50 | IC50 | pIC50 | IC50 | pIC50 | IC50 | pIC50 | IC50 | pIC50 | IC50 | pIC50 | IC50 |
PARP1 | FL | 8.48±0.14 | 3.3 | 7.79±0.08 | 16.7 | 8.86±0.12 | 1.4 | 8.95±0.18 | 1.1 | 8.50±0.08 | 3.2 | 7.96±0.10 | 10.9 | 6.84±0.68 | 145 |
PARP1 | Zn3-C | 6.45±0.07 | 354 | 7.16±0.10 | 18.9 | 6.52±0.08 | 301 | 6.32±0.07 | 481 | ||||||
PARP1 | ART | 7.45±0.08 | 35.2 | 6.88±0.14 | 132 | 7.99±0.07 | 10 | 7.40±0.12 | 39.8 | 7.22±0.13 | 61 | ||||
PARP2 | FL | 7.76±0.10 | 17.5 | 7.81±0.16 | 15.3 | 7.91±0.11 | 12.3 | 8.38±0.06 | 4.1 | 7.55±0.18 | 28.2 | 7.48±0.06 | 33.5 | 5.97±0.05 | 1000 |
PARP2 | ART | 6.86±0.07 | 137 | 6.60±0.12 | 251 | 6.86±0.09 | 138 | 6.42±0.06 | 382 | ||||||
PARP3 | FL | 5.67±0.11 | 2040 | 6.53±0.18 | 296 | 6.64±0.10 | 230 | 7.20±0.04 | 62.8 | 6.39±0.09 | 512 | 5.84±0.15 | 1430 | 5.89±0.21 | 1300 |
PARP4 | ART | 5.46±0.09 | 3500 | 6.35±0.14 | 446 | 6.39±0.11 | 410 | 6.59±0.14 | 254 | 6.08±0.09 | 839 | 6.12±0.18 | |||
TNKS1 | SAM-ART | 4.97±0.06 | 10740 | 6.49±0.13 | 322 | 6.84±0.05 | 144 | 5.51±0.12 | 3100 | ||||||
TNKS1 | ART | 5.63±0.08 | 2355 | 5.91±0.06 | 1230 | 5.77±0.05 | 1690 | ||||||||
TNKS2 | ART | 4.62±0.10 | 24000 | 5.29±0.96 | 5130 | 5.3±0.04 | 2340 | 6.97±0.07 | 108 | 6.05±0.05 | 890 | 5.53±0.10 | 2900 | ||
PARP10 | FL | 5.72±0.15 | 1900 | 5.71±0.07 | 1900 | 5.03±0.09 | 9300 | 5.11±0.08 | 7800 | 6.25±0.11 | 570 | 5.23±0.10 | 5800 | 5.15±0.08 | 7100 |
PARP10 | ART | 4.36±0.07 | 43800 | 5.48±0.04 | 3300 | 5.90±0.07 | 1250 | 5.64±0.05 | 2310 | 5.17±0.15 | 6800 | ||||
PARP12 | ART | 4.23±0.27 | 59400 | 6.10±0.15 | 79 | 4.99±0.04 | 10050 | 5.18±0.15 | 6650 | 6.65±0.11 | 230 | ||||
PARP14 | ART | 4.05±0.26 | 89000 | 5.76±0.08 | 17300 | n.i. | n.i. | 4.60±0.04 | 25500 | 5.05±0.05 | 8830 | 5.38±0.05 | 4200 | 5.24±0.09 | 5700 |
PARP15 | ART | n.i. | n.i. | 4.54±0.16 | 29200 | 4.75±0.06 | 17600 | 4.32±0.16 | 47400 | 4.49±0.07 | 32600 | 5.05±0.15 | 9000 | ||
PARP16 | FL | n.i. | n.i. | 5.29±0.17 | 5100 | 5.73±0.15 | 1900 | n.i. | n.i. |
IC50 values in nanomolar (nM)