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PARP inhibitors block poly(ADP-ribose) polymerases (PARPs), enzymes that mark DNA damage and recruit repair proteins. PARP1 and PARP2 bind DNA single-strand breaks and attach poly(ADP-ribose) chains to themselves and to nearby chromatin proteins. Cells lacking breast cancer susceptibility proteins 1 or 2 (BRCA1, BRCA2), and therefore defective in homologous recombination, are highly sensitive to PARP inhibition. This synthetic lethal relationship, reported in 2005, has shaped much of the research on DNA repair inhibitors. Olaparib, niraparib, veliparib and talazoparib target the catalytic domains of PARP1 and PARP2, and 3-aminobenzamide is an early benzamide inhibitor. XAV 939 instead inhibits tankyrases 1 and 2 (TNKS1, TNKS2), which stabilizes axin in Wnt signaling studies.
PARP7-IN-18 is a potent selective inhibitor of PARP7, exhibiting an IC50 value of 0.11 nM. This compound demonstrates significant anticancer activity, making it a valuable tool for research applications focused on cancer biology and the therapeutic potential of targeting PARP7. Its favorable pharmacokinetic properties further enhance its utility in in vivo studies and drug development.
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NU 1085 is a potent poly(ADP-ribose) polymerase (PARP) inhibitor with an impressive Ki of 6 nM. This compound exhibits significant cytotoxicity towards cancer cells, with an LC50 between 83-94 μM. Additionally, NU 1085 has the potential to enhance the anticancer effects of Temozolomide, making it a valuable tool for cancer research, particularly in the study of lung cancer and other malignancies.
PARP1-IN-20, a selective PARP1 inhibitor, exhibits a potent inhibitory effect with an IC50 of 4.62 nM. This compound demonstrates minimal PARP-Trapping activity compared to other known inhibitors, including a significant threshold of >100 μM in the MDA-MB-436 cell line. PARP1-IN-20 is suitable for research applications focused on cancer therapy and DNA damage repair mechanisms.
ADP-ribose/PARP-IN-1 is a conjugated compound that combines disease-targeting moieties with PARP inhibitor functionality. This reagent selectively delivers PARP inhibitors to tumor cells, facilitating the inhibition of PARP enzymes that are critical for DNA damage repair. The presence of a cleavable linker ensures the release of the PARP inhibitor under specific conditions, while the chelator component enables the accumulation of radionuclides that exert cytotoxic effects. ADP-ribose/PARP-IN-1 is a valuable tool for research into prostate cancer and other malignancies characterized by PARP dependency.
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LT-626 is a potent poly(ADP-ribose) polymerase (PARP) inhibitor, with an IC50 of 1.60 nM. This inhibitor effectively reduces cellular poly(ADP-ribose) synthesis, demonstrating an EC50 of 17.9 nM, and displays enhanced cytotoxicity in colorectal cancer cells with MRE11 mutations. Additionally, LT-626 exhibits synergistic effects when combined with chemotherapeutic agents such as Cisplatin, Oxaliplatin, and SN-38, making it a valuable tool for colorectal cancer research applications.
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TNKS-2-IN-4 is a selective inhibitor of TNKS-2, demonstrating an IC50 of 19 nM. This compound exhibits significant anticancer activity specifically against colorectal cancer, making it a valuable tool for research in cancer biology and therapeutic development. Its selective inhibition of TNKS-2 highlights its potential for studying the mechanisms of tumor progression and treatment responses.
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RBN010860 is a potent inhibitor of PARP7, exhibiting an IC50 value of less than 0.1 μM. This reagent serves as a valuable tool for investigating the role of PARP7 in cancer biology, enabling researchers to explore its potential as a therapeutic target in oncological studies.
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PARP7-IN-12 is a potent inhibitor of PARP7, exhibiting an IC50 value of 7.836 nM. This compound demonstrates significant potential in cancer research by modulating poly(ADP-ribose) polymerase activity, which is associated with DNA damage response pathways. PARP7-IN-12 may serve as an effective tool for elucidating the role of PARP7 in tumor biology and for developing therapeutic strategies targeting PARP-related pathways in cancer.
PARP1-IN-6 is a dual inhibitor of tubulin and PARP-1, displaying IC50 values of 0.94 μM and 0.48 μM, respectively. This compound demonstrates significant biological activity by disrupting cellular processes mediated by both targets, making it a valuable tool for cancer research. PARP1-IN-6 is particularly useful in studies investigating the roles of PARP inhibition in DNA repair mechanisms and cytoskeletal dynamics.
Synonyms: 6,7-Dimethoxy-2-(1-piperazinyl)-4-quinazolinamine hydrochloride
DPQ hydrochloride is a potent and selective inhibitor of PARP-1 (poly(ADP-ribose) polymerase 1), effectively blocking PARP-1-mediated DNA damage repair and reducing NAD+/ATP consumption. This compound demonstrates significant anti-inflammatory properties by inhibiting the activation of the NF-κB pathway, leading to a decrease in pro-inflammatory cytokines such as TNF-α and IL-6, as well as mitigating oxidative stress. DPQ hydrochloride is ideal for research applications related to inflammation and can be utilized in studies of conditions such as acute lung injury, myocardial infarction, and neurodegenerative diseases.
Lotixparib is a potent inhibitor of poly(ADP-ribose) polymerase-1 (PARP-1), a key enzyme involved in DNA damage repair. This compound demonstrates cytoprotective effects, offering potential therapeutic applications in retinal diseases. Lotixparib is valuable for research focused on PARP-1-related conditions and mechanisms underlying DNA repair pathways.
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Vrucaparib-TP4 is a PROTAC-type degrader that targets PARP1. It facilitates the ubiquitination and subsequent degradation of PARP1, making it a valuable tool in cancer research. This compound is particularly useful for investigating the role of PARP1 in tumor biology and evaluating therapeutic strategies that exploit the degradation pathway for potential anti-tumor effects.
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PARP7-IN-23 is a potent inhibitor of Poly(ADP-ribose) polymerase 7 (PARP7) with an EC50 of 0.915 nM for phosphorylated STAT1 (pSTAT1) in NCI-H1373 cells. This compound demonstrates significant inhibitory activity, which positions it as a valuable tool for cancer research, particularly in studies involving STAT1 signaling pathways and therapeutic interventions targeting PARP7.
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PARP1-IN-21 is a potent inhibitor of PARP1, exhibiting an IC50 of less than 10 nM. This compound effectively disrupts the poly(ADP-ribose) polymerase 1 enzymatic activity, leading to the inhibition of DNA repair processes. It is primarily utilized in research applications focused on cancer biology and therapeutic development, particularly in the exploration of combination therapies for tumors with defective homologous recombination.
PARP1-IN-43 is a potent PARP1 inhibitor with an IC50 of 5 nM, exhibiting effective penetration across the blood-brain barrier. This compound is primarily utilized in research focused on homologous recombination-deficient central nervous system (CNS) tumors, facilitating the exploration of targeted therapies in oncology. Its ability to selectively inhibit PARP1 makes it a valuable reagent for investigating DNA repair mechanisms and their implications in cancer biology.
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PARP1-IN-39 is a potent inhibitor of PARP1, exhibiting an IC50 of 0.22 nM, and an IC50 of 1.57 nM in human breast cancer cells. This compound is valuable for investigating cancers associated with DNA repair deficiencies, including those linked to BRCA1/2 mutations, and is applicable in studies of breast, ovarian, pancreatic, and prostate cancers. PARP1-IN-39 facilitates research into targeted therapies that exploit the vulnerabilities of cancer cells with defective DNA repair mechanisms.
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Synonyms: TNKS-IN-22
TNKS 22 is a selective inhibitor of tankyrase 1 and tankyrase 2. It demonstrates potent inhibitory activity, with IC50 values of 0.1 nM and 4.1 nM for TNKS1 and TNKS2, respectively. This compound serves as a valuable tool for research into the roles of tankyrases in cellular processes such as the Wnt signaling pathway and telomere regulation. Applications include studies in cancer biology and therapeutic development targeting poly(ADP-ribose) polymerase pathways.
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KCL-440 is a potent PARP inhibitor that effectively penetrates the central nervous system, exhibiting an IC50 of 68 nM for PARP-1 inhibition. This compound is primarily utilized in research exploring DNA repair mechanisms, cancer therapy, and neurodegenerative disease models, making it a valuable tool for studying therapeutic strategies targeting cellular stress responses.
PARP7-probe-1 is a biotinylated chemiluminescent probe specifically designed to bind to the active site of PARP7. This reagent allows for the investigation of PARP7's enzymatic activity and its role in various biological processes. PARP7-probe-1 is suitable for applications involving protein interactions and the study of cellular mechanisms associated with PARP7 function.
TIPARP-IN-1 is a selective inhibitor of PARP7 (TIPARP) with an IC50 of 2.15 nM. By inhibiting TIPARP, this compound restores the interferon signaling pathway in tumors, effectively enhancing the anti-tumor immune response within the tumor microenvironment while minimizing systemic cytokine production. TIPARP-IN-1 is an important tool for investigating the role of PARP7 in head and neck squamous cell carcinoma.
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4-Aminonaphthalimide is a potent inhibitor of poly(ADP-ribose) polymerase (PARP), a key enzyme involved in DNA repair processes. This compound enhances the cytotoxic effects of γ-radiation in cancer cells, making it a valuable tool for studies focused on cancer therapy and radiation biology. Its dual function as a PARP inhibitor and radiation sensitizer positions 4-Aminonaphthalimide as an important reagent for research applications in oncology and therapeutic resistance.
PARP1-IN-51 is a potent inhibitor of the enzyme PARP1, which plays a critical role in DNA repair mechanisms. This compound exhibits significant biological activity by disrupting the PARP1-mediated repair of single-strand breaks, ultimately leading to cancer cell apoptosis. PARP1-IN-51 is particularly valuable for research in oncology, including studies focused on breast cancer and other malignancies with defective DNA repair pathways.
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PARP1-IN-37 is a selective inhibitor of poly(ADP-ribose) polymerases 1 and 2 (PARP1/2), exhibiting an IC50 of 24 nM for PARP1. This compound effectively inhibits PARP activity in cellular assays with an EC50 of 3.7 μM. PARP1-IN-37 is particularly relevant for investigations into BRCA-mutated tumors, including breast and ovarian cancers, making it a valuable tool for cancer research and therapeutic development.
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Tankyrase-IN-3 is a selective inhibitor of tankyrase 1 (TNKS1), demonstrating an IC50 value of 22 nM. This compound plays a significant role in the regulation of Wnt signaling pathways and cellular processes related to tumorigenesis. Tankyrase-IN-3 is primarily utilized in cancer research, offering insights into the therapeutic mechanisms targeting TNKS1 in various malignancies.
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PARP1-IN-18 is a potent inhibitor of the poly(ADP-ribose) polymerase 1 (PARP1) enzyme, demonstrating an IC50 value of 2.7 nM. This compound exhibits significant anticancer activity, making it a valuable tool for research applications targeting DNA repair mechanisms and cancer therapeutics. PARP1-IN-18 can be utilized to explore PARP-mediated cellular processes and evaluate its potential in combination therapies for various malignancies.
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