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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-24 is a highly potent inhibitor of PARP7, exhibiting an EC50 of 0.375 nM for pSTAT1 in NCI-H1373 cells. This compound is poised for significant contributions to cancer research, facilitating the study of PARP7's role in tumor biology and potential therapeutic interventions. Its strong inhibitory activity makes it a valuable tool for exploring the molecular mechanisms underlying cancer progression and treatment responses.
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PARP-1-IN-23 is a selective inhibitor of poly(ADP-ribose) polymerase 1 (PARP-1), exhibiting an IC50 of 12.38 nM. This compound demonstrates significant antitumor activity in vivo, making it a valuable tool for studying the mechanisms of cancer progression and treatment. Its inhibition of PARP-1 suggests potential applications in enhancing the efficacy of chemotherapy and targeting cancer cell survival pathways.
Synonyms: IMP4297 hydrochloride; JS109 hydrochloride
Senaparib hydrochloride is a selective inhibitor of PARP1 and PARP2, demonstrating significant anti-tumor activity. This compound is particularly effective in the treatment of advanced ovarian cancer, making it relevant for research focused on cancer therapeutics and mechanisms of tumor progression. Its ability to interfere with DNA repair pathways positions Senaparib hydrochloride as a valuable tool in understanding the efficacy of PARP inhibition in oncology.
PARP-2/1-IN-2 is a potent inhibitor of poly (ADP-ribose) polymerases 1 and 2, exhibiting Kis of 2 nM and 5 nM, respectively. It demonstrates a biological activity with an EC50 of 3 nM in cell-based assays assessing PARP activity. This compound is valuable for research focused on cancer therapeutics, DNA repair mechanisms, and the role of PARP in various cellular processes.
PARP1-IN-28 is a potent inhibitor of Poly(ADP-ribose) polymerase 1 (PARP1), a crucial enzyme involved in DNA repair and cellular response to stress. This compound exhibits significant anti-proliferative activity and is particularly relevant in cancer research, enabling studies on tumor cell viability and resistance mechanisms. Its application extends to assessing the efficacy of combination therapies in oncology, particularly in contexts involving homologous recombination deficiency.
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PARP1/2-IN-4 is a selective inhibitor of PARP1 and PARP2 enzymes, which play crucial roles in DNA repair processes via the base excision repair pathway. This compound exhibits significant potential in preclinical research for cancer therapy by enhancing the efficacy of DNA-damaging agents and promoting synthetic lethality in tumors with deficient DNA repair mechanisms. It is a valuable tool for studying DNA repair pathways and evaluating therapeutic strategies in oncology research.
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PARP10-IN-2 is a selective inhibitor of the mono-ADP-ribosyltransferase PARP10, exhibiting an IC50 of 3.64 µM in human PARP10 assays. This compound also effectively inhibits PARP2 and PARP15, with IC50 values of 27 µM and 11 µM, respectively. PARP10-IN-2 is valuable for research applications focusing on cellular processes influenced by ADP-ribosylation and has potential implications in cancer and neurodegenerative disease studies.
KMR-206 is a selective inhibitor of PARP7, demonstrating an IC50 of 13.7 nM. This compound enhances the activation of STAT1 and phosphorylated STAT1, thereby promoting type I interferon signaling through STING degradation. KMR-206 exhibits notable anticancer activity, particularly against lung adenocarcinoma, and serves as a valuable tool for investigating its effects in colon cancer research.
YCH1899 is an orally active PARP inhibitor, demonstrating a potent IC50 of less than 0.001 nM for PARP1/2. This compound exhibits significant antiproliferative effects against Capan-1 cells resistant to Olaparib and Talazoparib, with IC50 values of 0.89 nM and 1.13 nM, respectively. YCH1899 also presents favorable pharmacokinetic properties in rat models, making it a valuable tool for research in cancer therapeutics and resistance mechanisms.
PARP1-IN-29 is a potent PARP-1 inhibitor with an IC50 of 6.3 nM, demonstrating strong efficacy in modulating DNA damage repair pathways. Labeled with [18F], this compound is suitable for positron emission tomography (PET) imaging, allowing for targeted visualization of PARP-1 activity in tumors. Its applications extend to oncology and imaging research, providing valuable insights into cancer biology and treatment response.
Synonyms: 5-Aminoisoquinolin-1-one
5-AIQ (5-Aminoisoquinolin-1-one) is a selective inhibitor of PARP-1, a key protein involved in DNA repair mechanisms. This compound exhibits significant potential in reducing tissue injury resulting from ischemia-reperfusion of the liver. 5-AIQ is useful for research applications focused on understanding ischemia-reperfusion injury and developing therapeutic strategies for liver protection.
G-631 is a potent tankyrase (TNKS1/TNKS2) inhibitor that modulates the Wnt/β-catenin signaling pathway by stabilizing AXIN. This compound has demonstrated weak anti-tumor activity in preclinical models of colorectal cancer. G-631 is suitable for research applications focused on the mechanisms of cancer progression and the exploration of therapeutic strategies for colorectal cancer.
UKTT15 is an allosteric inhibitor of the enzyme PARP1. It exhibits significant inhibitory activity against PARP1, influencing DNA repair mechanisms and cellular response to DNA damage. UKTT15 is useful in research focused on cancer biology, particularly in studies evaluating the therapeutic potential of PARP inhibition in cancer treatment and the modulation of DNA repair pathways.
TNKS-2-IN-2 is a selective inhibitor targeting tankyrase 2 (TNKS2), exhibiting an IC50 of 22 nM. This compound plays a crucial role in the regulation of RNA processing and signaling pathways by inhibiting poly(ADP-ribose) polymerase activity. TNKS-2-IN-2 is utilized in research exploring cancer biology and cellular senescence, offering insights into the therapeutic potential of targeting TNKS2 in various disease models.
EB-47 is a selective inhibitor of PARP-1 (ARTD-1) with an IC50 value of 45 nM, demonstrating its strong inhibition profile. It also exhibits modest potency against ARTD5 with an IC50 of 410 nM. Structurally, EB-47 mimics the substrate NAD+, extending from the nicotinamide to the adenosine subsite, making it a valuable tool for studying DNA repair mechanisms and related cancer research applications.
AZ3391 is a selective inhibitor of the PARP enzyme family, which is critically involved in cellular processes including DNA repair, chromatin remodeling, and cell cycle regulation. As a quinoxaline derivative, AZ3391 demonstrates significant potential for investigating neurodegenerative diseases and conditions affecting the central nervous system, particularly in the brain and spinal cord. This compound is valuable for research applications focused on understanding the mechanisms underlying DNA damage response and related pathologies.
Synonyms: JPI-289 free base
Amelparib is a selective inhibitor of PARP-1, exhibiting potent activity with an IC50 of 18.5 nM for PARP-1 inhibition and 10.7 nM for cellular PAR formation. This orally active and water-soluble compound demonstrates potential neuroprotective effects, making it a valuable tool for research in the field of acute ischemic stroke. Amelparib's ability to modulate PARP-1 activity offers insights into its therapeutic roles in neuroprotection and cellular repair mechanisms.
PARP1-IN-7 is a selective inhibitor of poly(ADP-ribose) polymerase-1 (PARP1), primarily functioning to disrupt DNA repair mechanisms in cancer cells. By inhibiting PARP1 activity, it enhances the cytotoxic effects of DNA-damaging agents, making it a valuable tool in cancer research. Its applications include studying mechanisms of tumorigenesis, evaluating synthetic lethality in cancer therapies, and exploring potential combinations with other anticancer agents.
TNKS-2-IN-1, a potent TNKS-2 inhibitor, selectively targets tankyrases 1 and 2. It exhibits inhibitory activity with IC50 values of 259 nM for TNKS-1 and 1100 nM for TNKS-2. This compound is utilized in research applications investigating cellular processes related to telomere maintenance, Wnt signaling, and cancer therapy.
Synonyms: GPI 21016
E7016 is a potent orally bioavailable inhibitor of PARP (Poly(ADP-ribose) polymerase). By inhibiting DNA repair mechanisms, E7016 enhances the radiosensitivity of tumor cells both in vitro and in vivo, making it a promising candidate for cancer therapeutics. This compound is useful in research applications focused on cancer treatment strategies involving DNA damage response and repair pathways.
ART-IN-1 is a selective inhibitor of poly(ADP-ribose) polymerases (PARPs), with IC50 values of 19 µM for PARP2, 22 µM for TNKS2, 2.4 µM for PARP10, greater than 100 µM for PARP14, and 1.1 µM for PARP15. This compound is utilized in research focused on DNA damage repair mechanisms and cancer therapeutics, making it a valuable tool for studying PARP-related pathways and their implications in various diseases. ART-IN-1 is instrumental in elucidating the role of PARP inhibition in enhancing the efficacy of chemotherapy and targeted therapies.
KSQ-4279 (gentisate) is a potent inhibitor of USP1 and selectively targets PARP1. This compound demonstrates significant potential in cancer research, showcasing its ability to disrupt key pathways involved in tumor progression and repair mechanisms. Its unique inhibitory properties make it a valuable tool for studying the molecular underpinnings of various cancer types and developing targeted therapeutic strategies.
iVeliparib-AP6 is a proteolysis-targeting chimera (PROTAC) that functions as a potent inhibitor of PARP1 and PARP2. It demonstrates DC50 values for PARP1 and PARP2 degradation at 36 nM and 63 nM, respectively, with IC50 values of 69 nM and 21 nM. The compound contains a Veliparib-based PARP inhibitor warhead linked to a CRBN E3 ligase binder, utilizing Thalidomide to recruit CRBN E3 ubiquitin ligase, thereby facilitating effective degradation of PARP2. This innovative mechanism positions iVeliparib-AP6 as a valuable tool for studying PARP-related pathways and therapeutic strategies in cancer research.
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TNKS1/2-IN-1 is a potent inhibitor of tankyrase 1 and 2, demonstrating pIC50 values between 7.1 and 8.2. This compound effectively modulates the activity of TNKS1/2, making it a valuable tool for research into cancer, fibrosis, and other hyperproliferative diseases. Its selective inhibition offers insights into the biological pathways regulated by tankyrases, facilitating the exploration of therapeutic strategies targeting these conditions.
PARP-1-IN-4 is a selective inhibitor of PARP-1, exhibiting an IC50 value of 302 μM. This compound is utilized in research focused on lung adenocarcinoma, where inhibiting PARP-1 activity may contribute to understanding cancer pathophysiology and therapeutic strategies. Its specificity for PARP-1 makes it a valuable tool in studying DNA repair mechanisms and their impact on cancer cell proliferation and survival.
