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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.
Synonyms: IDX-1197
Venadaparib is a selective and potent inhibitor of PARP1 and PARP2, exhibiting IC50 values of 1.4 nM and 1.0 nM, respectively. This orally active compound effectively impedes the repair of DNA single-strand breaks (SSB). Venadaparib is relevant for research applications targeting solid tumors and investigating the role of PARP in DNA damage response pathways.
1,5-Isoquinolinediol is a potent inhibitor of poly(ADP-ribose) polymerase (PARP), exhibiting an IC50 range of 0.18-0.37 μM. This compound is particularly effective in mitigating diabetes-induced oxidative stress through the inhibition of NADPH oxidase in retinal tissues. Its ability to modulate cellular responses to oxidative stress makes it a valuable tool for research into diabetes-related complications and neuroprotection.
Synonyms: M2912
MSC2504877 is a potent and orally active tankyrase inhibitor, exhibiting IC50 values of 0.0007 µM for TNKS, 0.0008 µM for TNKS2, and 0.54 µM for PARP1. This compound effectively increases AXIN2 and TNKS protein expression while decreasing β-catenin levels, indicating its role in the regulation of key signaling pathways. MSC2504877 demonstrates significant anti-tumor activity, making it a valuable tool for cancer research and therapeutic studies targeting the Wnt signaling pathway.
N-Descyclopropanecarbaldehyde Olaparib is a potent PARP inhibitor, serving as an analogue of Olaparib with a DOTA moiety. This compound is utilized in the synthesis of novel dual EGFR and PARP PROTAC, designated as DP-C-4. Additionally, N-Descyclopropanecarbaldehyde Olaparib can be radiolabeled with F-18 or fluorophores, enabling its application in positron emission tomography (PET) and optical imaging for various tumor types.
Synonyms: Olaparib-bodipy FL
PARPi-FL is a small-molecule fluorescent inhibitor targeting PARP1. It binds selectively to PARP1 and is utilized as a fluorescent imaging agent, facilitating tumor detection, diagnosis, and surgical guidance. This compound serves as a valuable tool in cancer research, offering insights into PARP1 activity in various biological contexts.
PARP7-IN-15 is a selective inhibitor of PARP7, exhibiting an IC50 of 0.56 nM. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. Its potency in inhibiting PARP7 can facilitate studies focused on DNA repair mechanisms and cancer cell proliferation.
Synonyms: JPI-547/OCN-201
Nesuparib is a potent inhibitor of PARP 1 and 2, as well as Tankyrase 1 and 2, with IC50 values of 5 nM, 1 nM, and 2 nM, respectively. This orally bioavailable compound demonstrates significant antitumor activity, making it a valuable tool for researching advanced solid tumors. Its selective inhibition of critical DNA repair pathways highlights its potential in cancer therapy and provides important insights into targeted treatment strategies.
AZ9482 is a potent inhibitor of PARP1, PARP2, and PARP6, exhibiting IC50 values of 1 nM for both PARP1 and PARP2, and 640 nM for PARP6. This compound effectively disrupts the DNA repair pathway in cancer cells, making it a valuable tool for studying cellular response to DNA damage. AZ9482 is appropriate for applications in cancer research, particularly in the context of synthetic lethality and therapeutic resistance.
PARP7-IN-16 is a selective and orally bioavailable inhibitor of PARP-1, PARP-2, and PARP-7, exhibiting IC50 values of 0.94 nM, 0.87 nM, and 0.21 nM, respectively. This compound serves as a valuable research tool for investigating the roles of PARP enzymes in cellular processes and their implications in oncogenesis. It is particularly relevant for studies focusing on breast cancer and prostate cancer, providing insights into therapeutic strategies that target DNA repair mechanisms.
RK-582 is a potent tankyrase inhibitor that demonstrates antitumor activity with an IC50 of 36.1 nM against human tankyrase-1 and 39.2 nM against human tankyrase-2. This compound specifically targets APC-mutated colorectal cancer cells, where its efficacy is linked to levels of active β-catenin, while resistance is associated with PIK3CA mutations. RK-582 is valuable for research focused on colorectal cancer mechanisms and therapeutic strategies.
K-756 is a selective tankyrase (TNKS) inhibitor that effectively inhibits the ADP-ribosylation activity of TNKS1 and TNKS2, exhibiting IC50 values of 31 nM and 36 nM, respectively. This compound plays a significant role in the study of various cancer-related pathways and cellular processes influenced by tankyrase activity. K-756 is applicable in research focused on DNA repair mechanisms, cellular signaling, and the modulation of Wnt signaling pathways.
PARP10/15-IN-1 is a selective inhibitor targeting both PARP10 and PARP15, exhibiting IC50 values of 160 nM and 370 nM, respectively. This compound serves as a valuable tool for cancer research, enabling the investigation of PARP10 and PARP15's roles in tumorigenesis and therapeutic resistance. Its dual inhibitory properties facilitate studies aimed at understanding the molecular mechanisms of cancer progression and the potential for targeted therapies.
PARP10-IN-3 is a selective inhibitor of the mono-ADP-ribosyltransferase PARP10, exhibiting an IC50 of 480 nM against human PARP10. Additionally, it demonstrates significant inhibitory activity towards PARP2 and PARP15 with IC50 values of 1.7 μM. This compound serves as a valuable tool in research applications targeting the role of PARP enzymes in cellular processes and their implications in various diseases, including cancer.
Simmiparib is a potent and orally active inhibitor of PARP1 and PARP2, demonstrating IC50 values of 1.75 nM and 0.22 nM, respectively. This compound effectively induces the accumulation of DNA double-strand breaks and triggers G2/M phase arrest in homologous recombination repair-deficient cells, leading to apoptosis. Simmiparib exhibits significant antitumor activity in various cancer models, including xenografts in nude mice, making it a valuable tool for cancer research and therapeutic development.
PARP1-IN-5 dihydrochloride is a potent and selective inhibitor of PARP-1, with an IC50 of 14.7 nM. This compound exhibits low toxicity and is suitable for oral administration. PARP1-IN-5 dihydrochloride is primarily utilized in cancer research to investigate the role of PARP-1 in tumorigenesis and therapy resistance.
PARP7-IN-17 is a potent PARP7 inhibitor with an IC50 of 4.5 nM, demonstrating effective oral bioavailability. This compound exhibits significant antitumor activity, making it a valuable tool for research into cancer therapeutics and the biological role of PARP7 in tumorigenesis. Its selective inhibition of PARP7 may aid in the development of targeted cancer treatments.
PARP7-IN-22 is a potent PARP7 inhibitor with an IC50 of 0.6 nM. This compound is orally active and enhances type I interferon signaling in vitro, facilitating T cell infiltration into tumor tissues and significantly inhibiting tumor growth. PARP7-IN-22 is of particular interest for research in cancer immunotherapy, providing valuable insights into therapeutic strategies that target immune responses in oncology.
PARP7-IN-16 free base is a selective, orally active inhibitor of PARP-1, PARP-2, and PARP-7, exhibiting IC50 values of 0.94 nM, 0.87 nM, and 0.21 nM, respectively. This compound is valuable for investigating the role of PARP enzymes in DNA repair mechanisms and is particularly relevant in studies focused on breast and prostate cancer. Researchers can utilize PARP7-IN-16 free base to explore therapeutic strategies targeting these types of malignancies.
PARP1-IN-11 is a selective inhibitor of the poly(ADP-ribose) polymerase 1 (PARP1) enzyme, demonstrating a potent inhibitory activity with an IC50 value of 0.082 µM. This compound exhibits complete inhibition of PARP2 and significantly inhibits the activity of PARP3, as well as tankyrases TNKS1 and TNKS2. PARP1-IN-11 is valuable for research applications focused on DNA repair mechanisms, cancer therapeutics, and the study of cellular responses to genotoxic stress.
PARP1-IN-33 is a potent inhibitor of PARP1, exhibiting an IC50 of 0.41 nM. This compound demonstrates significant cytoprotective effects on retinal cells, with an EC50 of 0.02 nM in inhibiting MTS activity in H2O2-induced human retinal pigment epithelial cells. PARP1-IN-33 is valuable for research applications aimed at understanding retinal oxidative stress and developing therapeutic strategies for retinal diseases.
TIQ-A is a potent inhibitor of TNKS2 (tankyrase 2), exhibiting an IC50 of 24 nM. This compound has shown promise as an anti-ischemic agent, potentially modulating pathways involved in ischemic injury. It serves as a valuable tool for research focused on cellular stress responses and the role of TNKS2 in various diseases.
A-620223 is a potent inhibitor of PARP-1, exhibiting a Ki of 8 nM and an EC50 of 3 nM in whole cell assays. This compound demonstrates significant in vivo efficacy in murine models, particularly in the B16F10 melanoma model when used in combination with Temozolomide and in the MX-1 breast xenograft model with Cisplatin. A-620223 is suitable for research applications focusing on melanoma and breast cancer therapy.
Synonyms: AZD5305
Saruparib is a potent and selective PARP inhibitor, primarily targeting PARP1 with an IC50 value of 3 nM and PARP2 with an IC50 of 1400 nM. This orally active compound demonstrates significant anti-proliferative effects and is particularly effective in inhibiting the growth of cells exhibiting deficiencies in DNA repair mechanisms. Saruparib is commonly utilized in research focused on cancer treatment strategies, particularly in the context of homologous recombination repair-deficient tumors.
Synonyms: SHR3162; Fuzuloparib
Fluzoparib is a highly potent oral inhibitor of PARP1, demonstrating an IC50 of 1.46 ± 0.72 nM in cell-free enzymatic assays. This compound selectively targets homologous recombination repair (HR)-deficient cells while sensitizing both HR-deficient and HR-proficient cells to cytotoxic agents. With favorable pharmacokinetic properties in vivo, Fluzoparib is an important reagent for studying BRCA1/2-mutant relapsed ovarian cancer and related therapeutic strategies.
RBN012759 is a potent and selective inhibitor of PARP14, exhibiting an IC50 of less than 3 nM. It demonstrates 300-fold selectivity for monoPARPs and 1000-fold selectivity for polyPARPs. RBN012759 has been shown to diminish pro-tumor macrophage activity and trigger inflammatory responses in tumor explants, making it a valuable tool for research in cancer biology and immune modulation.
