Home DNA Damage/DNA Repair PARP

PARP inhibitors

PARP, one of the most abundant proteins in the nucleus, has the principal role in regulating the cellular processes that are most relevant in terms of pathophysiology and experimental therapy. PARP1 which is a 116-kDa protein consists of three main domains is the most important member of the PARP family and can be a DNA-damage sensor and signalling molecule because the ZINC FINGERS of PARP recognize singleand double-stranded DNA breaks. PARP can be cleaved into inactive fragments by caspases or matrix metalloproteinases (MMPs). The phosphorylation of PARP by protein kinase-C (PKC), through the inhibition of its DNA binding, also suppresses PARP activity. PARP, through physical interactions and/or catalytic actions, promotes activator protein-1 (AP1) and nuclear factor-κB (NF-κB)-dependent signal-transduction processes and can suppress the activation of the cytoprotective AKT pathway; therefore, the inhibition of PARP can suppress AP1 and NF-κB activation and induce AKT phosphorylation.

Other DNA Damage/DNA Repair Related Inhibitors

HDAC WRN Sirtuin Topoisomerase Telomerase DNA/RNA Synthesis MTH1 DNA alkylator High-mobility Group CRISPR/Cas9

Isoform-selective Products

Cat.No. Product Name Information Product Use Citations Product Validations
S1060 AZD2281 (Olaparib) 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.
Cell, 2025, 188(18):5081-5099.e27
Cancer Cell, 2025, 43(8):1530-1548.e9
Cancer Cell, 2025, 43(4):776-796.e14
Verified customer review of AZD2281 (Olaparib)
S7048 BMN-673 (Talazoparib) 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.
Mol Cancer, 2025, 24(1):217
Nat Commun, 2025, 16(1):8476
Nat Commun, 2025, 16(1):6972
Verified customer review of BMN-673 (Talazoparib)
S1180 XAV-939 XAV-939 (NVP-XAV939) selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition with IC50 of 11 nM/4 nM in cell-free assays, regulates axin levels and does not affect CRE, NF-κB or TGF-β.
Nat Biotechnol, 2025, 10.1038/s41587-025-02649-1
Nat Cell Biol, 2025, 27(8):1240-1255
Nat Cell Biol, 2025, NONE
Verified customer review of XAV-939
S9875 AZD5305 (Saruparib) 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).
Nature, 2024, 10.1038/s41586-024-07217-2
Nature, 2024, 628(8007):433-441
Nat Commun, 2024, 15(1):5822
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. This compound can form PARP–DNA complexes resulting in DNA damage, apoptosis, and cell death. Phase 3.
Nat Commun, 2025, 16(1):4239
Cancer Commun (Lond), 2025, 45(12):1706-1733.
Neuro Oncol, 2025, noaf061
Verified customer review of Niraparib (MK-4827)
S4948 Rucaparib (AG-014699) 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.
Cancer Res, 2025, 10.1158/0008-5472.CAN-24-2938
Cancer Lett, 2025, 613:217505
Stem Cell Res Ther, 2025, 16(1):548
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. This compound is inactive to SIRT2 and increases autophagy and apoptosis. Phase 3.
Nat Commun, 2025, 16(1):8476
Nat Commun, 2025, 16(1):1026
J Exp Med, 2025, 222(5)e20241184
Verified customer review of Veliparib (ABT-888)
S1098 Rucaparib phosphate Rucaparib phosphate 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. Phase 3.
Mol Cell, 2025, S1097-2765(25)00098-X
Cells, 2025, 14(14)1049
Cancer Res Commun, 2025, 10.1158/2767-9764.CRC-24-0515
Verified customer review of Rucaparib phosphate
S7300 PJ34 HCl PJ34 HCl is the hydrochloride salt of PJ34, which is a PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2.
Nucleic Acids Res, 2025, 53(20)gkaf1090
Cell Death Differ, 2025, 10.1038/s41418-025-01457-z
J Neuroinflammation, 2024, 21(1):235
Verified customer review of PJ34 HCl
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.
Cancer Res Commun, 2025, 10.1158/2767-9764.CRC-24-0515
Nat Commun, 2024, 15(1):9463
Nat Commun, 2024, 15(1):1041
Verified customer review of Niraparib tosylate

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