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 (212)
Related Products (212)
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Antibodies (2)
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PARP1/NAMPT-IN-1
0 ImagesPARP1/NAMPT-IN-1 is a potent and dual PARP1 and NAMPT inhibitor with IC50 values of 1.2 nM and 6.7 nM, respectively. PARP1/NAMPT-IN-1 can disrupt the homologous recombination repair (HRR) pathway, leading to the accumulation of DNA double-strand breaks (DSBs), inducing cell cycle arrest and apoptosis, and also has antimigratory effects. PARP1/NAMPT-IN-1 exhibits excellent antitumor effects in a breast cancer xenograft model. PARP1/NAMPT-IN-1 can be used for the study of triple-negative breast cancer (TNBC).
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PARP1/BRD4-IN-3
0 ImagesCat. No.: HY-169170PARP1/BRD4-IN-3 (compound HF4) is a potent BRD4 and PARP1 inhibitor with IC50 values of 1210, 2019 nM for BRD4, PARP1, respectively. PARP1/BRD4-IN-3 shows antiproliferative activities. PARP1/BRD4-IN-3 induces apoptosis and cell cycle arrest at G0/G1 phase. PARP1/BRD4-IN-3 causes DNA damage and reduces the protein expression of Rad51. PARP1/BRD4-IN-3 shows antitumor efficacy.
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PARP1 degrader-3
0 ImagesCat. No.: HY-189293PARP1 degrader-3 is a selective PARP1 degrader derived from Olaparib (HY-10162) bearing a bicyclo[1.1.1]pentane (BCP) hydrophobic tag. PARP1 degrader-3 degrades PARP1 with a DC50 of 4.31 μM. PARP1 degrader-3 induces PARP1 degradation primarily through the ubiquitin-proteasome system, and the HSP70/HSP90-associated protein quality control pathway may be involved in this process. PARP1 degrader-3 can be used for colorectal cancer-related research.
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OUL245
0 ImagesCat. No.: HY-W294889CAS No.: 1023814-45-0
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PARP1/c-Met-IN-1
0 ImagesCat. No.: HY-161372CAS No.: 2944101-99-7
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Castalagin
0 ImagesCat. No.: HY-N20707CAS No.: 24312-00-3Castalagin is an orally active natural product with multiple biological activities including antibacterial activity against bacteria and anti-leishmanial activity against Leishmania aethiopica. Castalagin exhibits inhibitory activity against PARP1 and DNA topoisomerase II, with an IC50 of 0.86 μM for bovine PARP1. Castalagin reduces poly (ADP-ribosyl) ation modification in cells. Castalagin binds to the cell envelope of Ruminococcus bromii, increases the ratio of CD8+/FOXP3+CD4+ T cells in the tumor microenvironment, and acts as a prebiotic to enhance the activity of anti-PD-1 therapy. Castalagin induces morphological changes in Leishmania aethiopica promastigotes and inhibits their proliferation. Castalagin inhibits PBP2a-mediated peptidoglycan layer stabilization, disrupts bacterial peptidoglycan assembly, and inhibits and disintegrates bacterial biofilms. Castalagin can be used in research related to diseases such as cancer, leishmaniasis, and bacterial infections.
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EGFR/PARP-1-IN-1
0 ImagesCat. No.: HY-183373EGFR/PARP-1-IN-1 is a dual EGFR and PARP-1 inhibitor with IC50 values of 64 nM and 12 nM, respectively. EGFR/PARP-1-IN-1 binds to the ATP-binding pocket of EGFR and interacts with the catalytic domain of PARP-1, inhibiting kinase and enzymatic activity via hydrogen bond formation with key residues in both targets. EGFR/PARP-1-IN-1 induces apoptosis through the endogenous mitochondrial pathway, arrests the cell cycle at the G2 phase, and inhibits cell proliferation. EGFR/PARP-1-IN-1 can be used for research on triple-negative breast cancer.
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PARP1/ERK IN-1
0 ImagesCat. No.: HY-181842PARP1/ERK IN-1 is a dual PARP1/ERK inhibitor, with a PARP1 IC50 of 0.9 nM and an ERK2 IC50 of 1.8 nM. PARP1/ERK IN-1 inhibits proliferation and migration of various cancer cell lines, and induces apoptosis and DNA damage. PARP1/ERK IN-1 suppresses tumor growth in mouse models of colorectal cancer, and reduces the expression of Ki‑67, BRCA1 and Rad51. PARP1/ERK IN-1 can be used in the research of colorectal cancer, triple-negative breast cancer and pancreatic cancer.
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Tubulin/PARP1-IN-1
0 ImagesCat. No.: HY-184277Tubulin/PARP1-IN-1 is a dual inhibitor of tubulin and PARP1, with IC50 values of 1.86 μM and 0.88 μM, respectively. Tubulin/PARP1-IN-1 arrests cancer cells at the G2/M phase, induces cancer cell apoptosis, enhances cellular DNA damage, inhibits tumor angiogenesis, reduces cancer cell colonization and dissemination, and exhibits antiproliferative activity against colorectal cancer cells. Tubulin/PARP1-IN-1 can be used in the research of colorectal cancer and colorectal cancer lung metastasis.
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PARP1-IN-22
0 ImagesCat. No.: HY-158681CAS No.: 3033649-17-8PARP1-IN-22 (compound 15) is a potent inhibitor of PARP1, with the IC50 of ＜ 10 nM.
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PARP1-IN-10
0 ImagesCat. No.: HY-149003CAS No.: 2494001-21-5
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SK-575-NEG
0 ImagesCat. No.: HY-147101CAS No.: 2523017-04-9SK-575-NEG (compound 28), a methylation counterpart of SK-575, is synthesized by methylation of the amino group of piperidine-2,6-dione in SK-575 as an control compound. SK-575-NEG is strongly bound to PARP1, with an IC50 of 2.64 nM. SK-575-NEG was completely ineffective in inducing PARP1 degradation in MDA-MB-436 and Capan-1 cells at concentrations up to 1 μM.
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PARP1-IN-55
0 ImagesCat. No.: HY-181459CAS No.: 3109617-69-5PARP1-IN-55 is a potent and selective PARP1 inhibitor with an IC50 value of 0.019 μM. PARP1-IN-55 exhibits anti-proliferative selective activity against MCF-7 breast cancer cells (IC50 = 3.6 μM). PARP1-IN-55 inhibits the PARP1-mediated DNA damage repair pathway, induces ROS accumulation, disrupts mitochondrial membrane potential, induced apoptosis and suppresses cancer cell migration, invasion, and colony formation. PARP1-IN-55 can be used for the study of breast cancer.
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PARP-1/HDAC-IN-1
0 ImagesCat. No.: HY-146160CAS No.: 3032621-10-3PARP-1/HDAC-IN-1 is a PARP-1/HDAC6 dual targeting inhibitor with IC50s of 68.90 nM and 510 nM, respectively. PARP-1/HDAC-IN-1 displays remarkable anticancer, anti-migration and anti-angiogenesis activities.
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PARP1/2-IN-3
0 ImagesCat. No.: HY-163817CAS No.: 3032451-58-1
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13'-Carboxy-δ-tocopherol
0 ImagesCat. No.: HY-N17653CAS No.: 1160974-35-513'-Carboxy-δ-tocopherol is a metabolite of long-chain vitamin E.13'-Carboxy-δ-tocopherol exhibits antiproliferative properties in cancer cells. 13'-Carboxy-δ-tocopherol activates caspase-3, caspase-9, causes PARP-1 cleavage, reduces mitochondrial membrane potential, increases ROS formation, and drives apoptosis.13'-Carboxy-δ-tocopherol can be used for the research of hepatocellular carcinoma.
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UNPD139734
0 ImagesCat. No.: HY-181140CAS No.: 116764-24-0UNPD139734 is a CDK-1 inhibitor and PARP-1 inhibitor that forms stable complexes with each target protein. UNPD139734 serves as a lead compound for structural optimization to develop dual-target anticancer agents targeting CDK-1 and PARP-1. UNPD139734 can be used for the research of breast cancer.
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PARP-1/2/7-IN-1
0 ImagesCat. No.: HY-161606CAS No.: 3034665-49-8PARP-1/2/7-IN-1 (compound 86) is a potent inhibitor of PARP-1/2/7, with the IC50 of ＜ 10 nM.
