PARP1
PARP1 (poly(ADP-ribose) polymerase 1) is a nuclear ADP-ribosyltransferase that functions as an early sensor of DNA strand breaks and catalyzes poly(ADP-ribosyl)ation to recruit DNA repair factors and coordinate chromatin remodeling at sites of genomic damage[1][2]. Mechanistically, PARP1 is a central component of the DNA damage response and plays critical roles in single-strand break repair and base excision repair through the recruitment of repair proteins such as XRCC1 and associated repair complexes[1][3]. Beyond local DNA repair, PARP1 contributes to genome surveillance by transmitting damage signals that influence repair pathway selection, replication stress responses, and maintenance of genomic stability[1][4]. In disease contexts, impaired PARP1-regulated repair can promote genomic instability, whereas elevated dependence on PARP1-mediated repair is a characteristic feature of multiple cancer models, particularly tumors with homologous recombination defects[4][5]. Compared with the related isoform PARP2, PARP1 accounts for the majority of DNA damage-induced poly(ADP-ribose) synthesis and displays distinct DNA-binding properties, including efficient recognition of single-strand DNA breaks, while PARP2 preferentially recognizes repair intermediates such as DNA gaps and flaps[3][6]. These functional distinctions support nonredundant contributions of PARP1 and PARP2 to the spatial and temporal organization of DNA repair pathways[3]. For experimental applications, PARP inhibitors have become widely used tools for investigating DNA damage responses and synthetic lethality, particularly in BRCA1/2-deficient tumor models, where suppression of PARP1-dependent repair enhances the accumulation of unrepaired DNA lesions and promotes selective cancer cell death[5][7].
References:
- [1]. Wang F, et al. PARPs and PARP inhibitors: molecular mechanisms and clinical applications. Mol Biomed. 2025 Dec 29;6(1):152. [Content Brief]
- [2]. Sciencedirect.topics.
- [3]. Yelamos J, et al. PARP-1 and PARP-2: New players in tumour development. Am J Cancer Res. 2011;1(3):328-346. Epub 2011 Jan 8. PMID: 21968702; PMCID: PMC3180065. [Content Brief]
- [4]. Petropoulos M, et al. Transcription-replication conflicts underlie sensitivity to PARP inhibitors. Nature. 2024 Apr;628(8007):433-441. [Content Brief]
- [5]. Rose M, et al. PARP Inhibitors: Clinical Relevance, Mechanisms of Action and Tumor Resistance. Front Cell Dev Biol. 2020 Sep 9;8:564601. [Content Brief]
- [6]. Szántó M, et al. Specific and shared biological functions of PARP2 - is PARP2 really a lil' brother of PARP1? Expert Rev Mol Med. 2024;26:e13.
- [7]. Underhill C, et al. A review of PARP inhibitors: from bench to bedside. Ann Oncol. 2011 Feb;22(2):268-79. [Content Brief]
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PARP1 Related Products (192)
Related Products (192)
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Antibodies (2)
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XAV-939
0 ImagesXAV-939 is a Tankyrase inhibitor. XAV-939 has inhibitory activity for TNKS1 and TNKS2 with IC50 values of 5 nM and 2 nM, respectively. XAV-939 also is an enhancer of osteoblastic differentiation of hMSCs. XAV-939 can be used for the research of conditions associated with activated Wnt signaling, such as cancer, fibrotic diseases and conditions associated with low bone formation.
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Talazoparib
0 ImagesSynonyms: BMN-673; LT-673
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iVeliparib-AP6
0 ImagesCat. No.: HY-130646CAS No.: 2472645-27-3iVeliparib-AP6 is a proteolysis-targeting chimera (PROTAC) molecule designed based on Veliparib (HY-10129), which targets PARP1/2. The DC50s of iVeliparib-AP6 for inducing the degradation of PARP1 and PARP2 are 36 nM and 63 nM, respectively, and its IC50s are 69 nM and 21 nM, respectively. iVeliparib-AP6 contains a Veliparib-based PARP inhibitor warhead linked to a CRBN E3 ligase binder; it uses Thalidomide (HY-14658) as a ligand to recruit CRBN E3 ubiquitin ligase and exerts the PARP2 degradation mechanism.
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2H-Indazole-7-carboxamide
0 ImagesCat. No.: HY-W973851CAS No.: 952479-70-8
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PJ34
0 ImagesPJ34 is a potent specific inhibitor of PARPl/2 with IC50 of 110 nM and 86 nM, respectively.
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IRF1-IN-1
0 ImagesIRF1-IN-1 (Compound I-2) is an IRF1 inhibitor. IRF1-IN-1 decreases the recruitment of IRF1 to the promoter of CASP1. IRF1-IN-1 inhibits cell death signaling pathway (i.e., cleavage of Caspase 1, GSDMD, IL-1 and PARP1). IRF1-IN-1 has a protective effect on ionizing radiation-induced inflammatory skin injury.
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Fluzoparib
0 ImagesSynonyms: SHR3162; FuzuloparibFluzoparib (SHR3162) is a potent and orally active PARP1 inhibitor (IC50=1.46±0.72 nM, a cell-free enzymatic assay) with superior antitumor activity. Fluzoparib selectively inhibits the proliferation of homologous recombination repair (HR)-deficient cells, and sensitizes both HR-deficient and HR-proficient cells to cytotoxic agents. Fluzoparib exhibits good pharmacokinetic properties in vivo and can be used for BRCA1/2-mutant relapsed ovarian cancer research.
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Niraparib hydrochloride
0 ImagesSynonyms: MK-4827 hydrochloride
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Rucaparib phosphate
0 ImagesSynonyms: AG-014699 phosphate; PF-01367338 phosphateRucaparib (AG014699) phosphate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib phosphate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib phosphate has the potential for castration-resistant prostate cancer (CRPC) research.
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Peiminine
0 ImagesSynonyms: Verticinone; RaddeaninePeiminine is a compound that can be isolated from Bolbostemma paniculatum (Maxim) Franquet (Cucurbitaceae family). Peiminine can induce apoptosis in human hepatocellular carcinoma HepG2 cells through both extrinsic and intrinsic apoptotic pathways. Peiminine has anti-inflammatory, anticancer, anti-osteoporosis, cardioprotective and other activities in many animal models.
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IRF1-IN-2
0 ImagesIRF1-IN-2 (Compound I-19) is an IRF1 inhibitor. IRF1-IN-2 decreases the recruitment of IRF1 to the promoter of CASP1. IRF1-IN-2 inhibits cell death signaling pathway (i.e., cleavage of Caspase 1, GSDMD, IL-1 and PARP1; inhibits the Pho of TKB1, upregulates GPX4 and downregulates FACL4). IRF1-IN-2 has a protective effect on ionizing radiation-induced inflammatory skin injury.
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Paris saponin VII
0 ImagesSynonyms: Chonglou Saponin VIIParis saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia.
