| S7048 |
Talazoparib (BMN 673) |
Talazoparib (BMN 673, LT-673) is a novel PARP inhibitor with IC50 of 0.57 nM for PARP1 in a cell-free assay. It is also a potent inhibitor of PARP-2, but does not inhibit PARG and is highly sensitive to PTEN mutation. Phase 3. |
Selective |
PARP1, IC50: 0.57 nM |
| S5195 |
Rucaparib Camsylate |
Rucaparib (Rubraca, AG014699, PF01367338) Camsylate is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. |
Selective |
PARP1, Ki: 1.4 nM |
| S4948 |
Rucaparib |
Rucaparib is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. |
Selective |
PARP1, Ki: 1.4 nM |
| S9875 |
Saruparib (AZD5305) |
Saruparib (AZD5305) is a highly selective and potent inhibitor of PARP1 with an IC50 of 3 nM in wild-type A549 lung cancer cells. AZD5305 shows no or minimal growth inhibitory effects in other cells (IC50s >10μM). |
Selective |
PARP1, IC50: 3 nM |
| S2178 |
AG-14361 |
AG14361 is a potent inhibitor of PARP1 with Ki of <5 nM in a cell-free assay. It is at least 1000-fold more potent than the benzamides. |
Selective |
PARP1, Ki: <5 nM |
| S8363 |
NMS-P118 |
NMS-P118 is a potent, orally available, and highly selective PARP-1 inhibitor endowed with excellent ADME and pharmacokinetic profiles, showing 150-fold selectivity for PARP-1 over PARP-2 (Kd 0.009 μM vs 1.39 μM, respectively). |
Selective |
PARP1, Kd: 0.009 μM |
| S0519 |
BYK204165 |
BYK204165 is a potent and selective inhibitor of the poly(ADP-ribose) polymerase (PARP). BYK204165 inhibits cell-free recombinant human PARP-1 (hPARP-1) with pIC50 of 7.35 and pKi of 7.05 and murine PARP-2 (mPARP-2) with pIC50 of 5.38, respectively. |
Selective |
hPARP-1, pIC50: 7.35; hPARP-1, pKi: 7.05 |
| S9360 |
4-Hydroxyquinazoline |
4-Hydroxyquinazoline (Quinazolin-4-ol, 4-Quinazolinol) is a PARP inhibitor with a high potency for PARP-1 with IC50 of 9.5 μM. |
Selective |
PARP1, IC50: 9.5 μM |
| S1087 |
Iniparib (BSI-201) |
Iniparib (BSI-201, NSC-746045, IND-71677) is a PARP1 inhibitor with demonstrated effectiveness in triple-negative breast cancer (TNBC). Phase 3. |
Selective |
|
| S8592 |
Pamiparib |
Pamiparib is a potent and selective inhibitor of PARP1 and PARP2 with IC50 values of 0.83 and 0.11 nM, respectively in biochemical assays. It shows high selectivity over other PARP enzymes. |
Pan |
PARP1, IC50: 0.83 nM |
| S2197 |
A-966492 |
A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively. |
Pan |
PARP1, Ki: 1 nM; PARP1, EC50: 1 nM |
| S8419 |
Stenoparib (E7449) |
Stenoparib (E7449, 2X-121, MGI25036) is an orally bioavailable, brain penetrable, small molecule dual inhibitor of PARP1/2 and also inhibits PARP5a/5b, otherwise known as tankyrase1 and 2 (TNKS1/2), important regulators of canonical Wnt/β-catenin signaling. It has IC50 values of 1.0 and 1.2 nM for PARP1 and 2, respectively. |
Pan |
PARP1, IC50: 1 nM |
| S9893 |
Venadaparib(IDX-1197) |
Venadaparib (IDX-1197), a potent PARP1/2 inhibitor with IC50 values of 1.4 nM and 1.0 nM respectively, prevents the repair of DNA single-strand breaks (SSB) and promotes the conversion of SSB to double-stranded breaks (DSB), which ultimately leads to synthetic lethality in cancer cells. |
Pan |
PARP1, IC50: 1.4 nM |
| S7625 |
Niraparib tosylate |
Niraparib tosylate is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM. Niraparib increases formation of PARP-DNA complexes resulting in DNA damage, apoptosis, and cell death. |
Pan |
PARP1, IC50: 3.8 nM |
| S2741 |
Niraparib (MK-4827) |
Niraparib (MK-4827) is a selective inhibitor of PARP1/2 with IC50 of 3.8 nM/2.1 nM, with great activity in cancer cells with mutant BRCA-1 and BRCA-2. It is >330-fold selective against PARP3, V-PARP and Tank1. Niraparib can form PARP–DNA complexes resulting in DNA damage, apoptosis, and cell death. Phase 3. |
Pan |
PARP1, IC50: 3.8 nM |
| S1060 |
Olaparib (AZD2281) |
Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1/2 with IC50 of 5 nM/1 nM in cell-free assays, 300-times less effective against tankyrase-1. Olaparib induces significant autophagy that is associated with mitophagy in cells with BRCA mutations. |
Pan |
PARP1, IC50: 5 nM |
| S1004 |
Veliparib (ABT-888) |
Veliparib (ABT-888, NSC 737664) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Veliparib increases autophagy and apoptosis. Phase 3. |
Pan |
PARP1, Ki: 5.2 nM |
| S6977 |
DR2313 |
DR2313 is a potent, selective, competitive and brain-penetrant inhibitor of poly(ADP-ribose) polymerase (PARP), with IC50s of 0.20 μM and 0.24 μM for PARP-1 and PARP-2, respectively. |
Pan |
PARP-1, IC50: 0.20 μM |
| S7438 |
ME0328 |
ME0328 is a potent and selective PARP inhibitor with IC50 of 0.89 μM for PARP3, about 7-fold selectivity over PARP1. |
Pan |
PARP1, IC50: 6.3 μM |
| S8038 |
UPF 1069 |
UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM. It is ~27-fold selective against PARP1. |
Pan |
PARP1, IC50: 8.0 μM |
