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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.
PARP1-IN-42 is a potent inhibitor of PARP1, exhibiting an IC50 value of less than 10 nM. This compound has demonstrated significant biological activity in disrupting DNA repair mechanisms, making it a valuable tool in cancer research. Its application can provide insights into the efficacy of PARP1 inhibition in various cancer models.
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TNKS1/2-IN-2 is a potent inhibitor of tankyrases, specifically targeting TNK1 and TNK2 with IC50 values of 4 nM and 63 nM, respectively, in enzymatic assays. This compound effectively inhibits the proliferation of A549 and H292 cell lines, demonstrating IC50 values of 39.5 nM and 12.8 nM. TNKS1/2-IN-2 is valuable for research applications focused on cancer, providing insights into tankyrase-related pathways and their influence on tumor growth.
OM-1700 is a potent tankyrase inhibitor, exhibiting IC50 values of 127 nM for tankyrase 1 and 14 nM for tankyrase 2. This compound effectively reduces cell proliferation in the colon cancer cell line COLO 320DM, with a GI50 of 650 nM. OM-1700 serves as a valuable tool for investigating the role of tankyrase in cancer biology and potential therapeutic applications.
ARTD10/PARP10-IN-1 is a potent and non-selective inhibitor of Poly(ADP-ribose) polymerases (PARPs), including ARTD7/PARP15, ARTD8/PARP14, ARTD10/PARP10, and ARTD1/PARP1, exhibiting IC50 values of 1.7 μM, 1.6 μM, 0.8 μM, and 4.4 μM respectively. This compound serves as a valuable tool for investigating the roles of mono-ADP-ribosylation and poly(ADP-ribosylation) in cellular processes. Its ability to inhibit multiple PARP family members makes it suitable for various research applications, including studies on DNA damage repair, cell proliferation, and apoptosis.
GPI 15427 is a selective inhibitor of poly (ADP-ribose) polymerase-1 (PARP-1), an enzyme implicated in inflammatory responses. This compound exhibits significant anti-inflammatory activity, particularly in rodent models of gut injury such as splanchnic artery occlusion shock and dinitrobenzene sulfonic acid-induced colitis. GPI 15427 effectively reduces inflammatory cell infiltration, mitigates histological damage, and prevents poly (ADP-ribose) accumulation in the ileum and colon. Its application in research is valuable for studying the role of PARP-1 in inflammatory diseases and potential therapeutic strategies.
PARP-1-IN-13 is a potent inhibitor of the enzyme PARP-1, exhibiting an IC50 value of 26 nM. This compound effectively disrupts DNA single-strand break repair mechanisms and exacerbates DNA double-strand breakage. Through the activation of the mitochondrial apoptosis pathway, PARP-1-IN-13 promotes apoptosis in cancer cells, making it a valuable tool for research in cancer therapy and DNA repair pathways.
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YCH3292 is a highly potent and selective inhibitor of PARP1 and PARP2, displaying an IC50 of less than 0.001 nM. This compound enhances the stability of PARP-DNA complexes and demonstrates significant antiproliferative effects by inducing double-strand breaks in DNA and increasing the expression levels of γH2AX, P-RPA32, and P-Chk1. YCH3292 effectively causes cell cycle arrest in the S and G2/M phases and promotes apoptosis in tumor cells, making it a valuable reagent for cancer research, particularly in exploring therapeutic strategies targeting PARP pathways. In vivo studies indicate that YCH3292 inhibits tumor growth in the MC38 xenograft mouse model.
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PARP-1-IN-1 is a highly selective and orally active inhibitor of PARP-1, exhibiting an IC50 of 0.96 nM. This compound demonstrates excellent tolerability and significant single-dose efficacy in the MDA-MB-436 xenotransplantation model. PARP-1-IN-1 is valuable for research in cancer biology and therapeutic applications targeting DNA repair mechanisms.
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PARP1-IN-54 is a selective inhibitor of the poly(ADP-ribose) polymerase 1 (PARP1) enzyme, which plays a crucial role in DNA repair mechanisms. This compound exhibits significant antitumor activity, making it a valuable tool in cancer research. Its inhibition of PARP1 can effectively enhance the therapeutic efficacy of DNA-damaging agents, and it is particularly relevant in studies focusing on cancer biology and treatment strategies involving synthetic lethality.
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PARP1-IN-47 is a highly selective inhibitor of the enzyme PARP1, demonstrating an IC50 value of less than 100 nM. By effectively blocking poly(ADP-ribosyl)ation, PARP1-IN-47 disrupts DNA damage repair mechanisms, leading to apoptosis in tumor cells. This compound holds potential for research applications in both solid tumors and hematological malignancies.
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PARP14 inhibitor 1 is a selective inhibitor of the poly(ADP-ribose) polymerase 14 (PARP14), demonstrating an IC50 of 5.52 nM. This compound exhibits anti-inflammatory properties and a half-life of 182 minutes in mouse liver microsomes. Its efficacy makes it a valuable tool for research in atopic dermatitis and related inflammatory disorders.
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NCT-TFP is a PARP probe designed for the identification of Poly(ADP-ribose) polymerases (PARP) inhibitors, facilitating research in cancer therapeutics and DNA repair mechanisms. This reagent enables the assessment of PARP activity and its modulation, which is critical for studying cellular responses to DNA damage. NCT-TFP is essential for investigating the role of PARP in various biological processes and for developing targeted therapies.
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PARP-1/2-IN-5 is a potent inhibitor of PARP-1 and PARP-2, with IC50 values of 118 nM and 11 nM, respectively. This compound is ideal for investigating its role in inflammatory diseases and neurodegenerative disorders, providing valuable insights into the therapeutic potential of PARP inhibition in these conditions. Researchers can utilize PARP-1/2-IN-5 to explore the molecular mechanisms underlying these diseases and assess potential treatment strategies.
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HYDAMTIQ is a potent inhibitor of PARP-1 and PARP-2, exhibiting an IC50 range of 29-38 nM. It demonstrates significant anticancer activity, targeting various malignancies such as ovarian, breast, prostate, pancreatic cancers, and glioblastoma multiforme. Additionally, HYDAMTIQ shows anti-inflammatory properties by reducing pulmonary PARP activity and can alleviate symptoms associated with allergen-induced cough and dyspnea. It also exhibits protective effects in in vivo models of cerebral ischemia, asthma, and cancer.
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Synonyms: (rac)-BMN-673; (rac)-LT-673
(rac)-Talazoparib is a potent inhibitor of PARP1 and PARP2, with Ki values of 1.2 nM and 0.87 nM, respectively. This orally active compound effectively inhibits cellular PARylation, demonstrating an EC50 of 2.51 nM. It induces DNA damage accumulation and significantly suppresses the proliferation of BRCA1/2-mutated cell lines, including MX-1 and Capan-1, with IC50 values of 0.3 nM and 5 nM, respectively. Additionally, (rac)-Talazoparib shows antitumor efficacy in various mouse models, making it a valuable tool for cancer research.
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PARP1-IN-8 is a potent inhibitor of the PARP1 enzyme, exhibiting an IC50 of 97 nM. This compound demonstrates significant anti-proliferative effects on the human lung adenocarcinoma cell line A549. It is suitable for research applications focused on cancer biology and the therapeutic potential of PARP1 modulation in oncology.
Itareparib is a PARP inhibitor that demonstrates significant antineoplastic activity by preventing the repair of DNA damage in cancer cells. This mechanism enhances cell death in tumor tissues, making it a valuable reagent for cancer research, particularly in studies involving homologous recombination repair deficiencies. Its application extends to exploring combination therapies and resistance mechanisms in oncology.
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TNKS-IN-2 is a potent and selective inhibitor of tankyrase (TNKS), exhibiting pIC50 values of 8.1 and 7.0 for TNKS and Wnt, respectively. This compound effectively modulates the Wnt signaling pathway by targeting TNKS, making it a valuable tool for research involving cellular growth and differentiation. TNKS-IN-2 is useful for studies investigating the role of tankyrases in cancer biology and other diseases associated with altered Wnt signaling.
Synonyms: ITK7
PARP11 inhibitor ITK7 is a potent and selective inhibitor targeting PARP11. It demonstrates strong inhibitory activity with an IC50 of 14 nM, making it a valuable tool for investigating the biological roles of PARP11. This compound can be utilized in research exploring cellular localization and the functional implications of PARP11 in various cellular contexts.
FeTMPyP is an orally active poly (ADP-ribose) polymerase (PARP) inhibitor that exerts protective effects against cell death and mitochondrial dysfunction. It significantly mitigates nitrotyrosine formation and depolarization of the mitochondrial transmembrane potential. FeTMPyP has been shown to alleviate homocysteine-induced nitrosative stress, improve functional and behavioral outcomes in neuropathic pain models, and reduce acute cerebral infarction in ischemic conditions. This compound is valuable for research related to renal aging, ischemic penumbra, and hyperglycemic strokes.
RBN-3143 is a potent NAD+-competitive inhibitor of PARP14, exhibiting an IC50 of 4 nM. This compound effectively inhibits PARP14-mediated ADP-ribosylation and stabilizes the enzyme in cellular contexts. RBN-3143 is ideal for investigating the role of PARP14 in lung inflammation and other related research applications.
DB008 is a selective inhibitor of the enzyme PARP16, demonstrating a potent inhibitory effect with an IC50 value of 0.27 μM. This compound features a membrane-permeable acrylamide electrophilic moiety, enabling specific targeting of PARP16. Additionally, DB008 contains an alkyne group that allows for click chemistry applications, specifically facilitating copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. Its unique properties make it a valuable tool for biochemical and molecular biology research involving PARP16.
DPQ is a selective inhibitor of PARP-1, effectively blocking PARP-1-mediated DNA repair mechanisms and reducing the consumption of NAD+ and ATP. This inhibition leads to a decrease in NF-κB pathway activation, resulting in lowered expression of pro-inflammatory cytokines such as TNF-α and IL-6, along with a reduction in oxidative stress levels. DPQ is applicable in research focused on inflammation-related conditions including acute lung injury, myocardial infarction, and neurodegenerative diseases.
Synonyms: IMP4297; JS109
Senaparib is a potent and selective inhibitor of PARP1 and PARP2, functioning through the inhibition of DNA repair pathways. Its mechanism disrupts the ability of cancer cells to repair DNA damage, leading to increased antitumor activity. Senaparib has demonstrated significant efficacy in various preclinical cancer models, making it a valuable tool for research in cancer biology and therapeutic development.
OM-153 is a potent inhibitor of tankyrase 1 and tankyrase 2 (TNKS1/2), exhibiting IC50 values of 13 nM and 2 nM, respectively. This compound effectively inhibits luciferase-based Wnt/β-catenin signaling reporter activity with an IC50 of 0.63 nM. Research applications include the investigation of Wnt/β-catenin signaling pathways and the effects of proliferation in COLO 320DM cells.
