PARP

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.

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.

PROTAC PARP1 degrader-1 is a potent degrader targeting PARP1 through the PROTAC mechanism. This compound facilitates the activation of the cGAS/STING immune pathway, enhancing T cell-mediated cytotoxicity against tumor cells. Additionally, by inhibiting DNA damage repair, PROTAC PARP1 degrader-1 promotes the accumulation of cytosolic DNA fragments, making it a valuable tool for research in cancer immunotherapy and the study of DNA repair mechanisms.

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.

RBN012811 is a selective PROTAC degrader that targets PARP14, facilitating its degradation through a ternary complex with cereblon by binding at the NAD+ site. With an IC50 of 10 nM, RBN012811 efficiently reduces endogenous PARP14 levels in various cell lines and primary human macrophages. This reduction is associated with decreased IL-10 production and IFN-β mRNA, alongside an increase in phosphorylated STAT1, thereby enhancing inflammatory signaling and inhibiting interferon-induced ADPr condensate formation. RBN012811 also influences viral replication dynamics, promoting HSV1 replication while diminishing VSV replication, making it valuable for research in cancer biology and viral infections.

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.

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.

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.

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.

Basroparib is a selective inhibitor of tankyrase (TNKS1/TNKS2) with IC50 values of 29.94 nM and 3.68 nM, respectively, and exhibits limited activity against PARP1 (IC50 > 10 μM). This compound stabilizes AXIN1/2 proteins and effectively disrupts the Wnt/β-catenin signaling pathway, leading to inhibition of tumor cell proliferation and induction of apoptosis. Basroparib is particularly relevant for research in colorectal cancer (CRC) models bearing KRAS mutations, such as G12V/G12D, and demonstrates potential to overcome resistance to MEK inhibitors, providing synergistic antitumor effects.

Benzamide is a potent inhibitor of poly(ADP-ribose) polymerase (PARP), demonstrating significant neuroprotective effects. It has been shown to protect against neurotoxicity induced by glutamate and methamphetamine in vitro. In vivo studies indicate that Benzamide can mitigate methamphetamine-induced dopamine depletions in mice without acute effects on striatal dopamine metabolism or body temperature regulation. Its dual role in neuroprotection and PARP inhibition makes it a valuable tool in neuropharmacology research.

OUL232 is a potent inhibitor of poly(ADP-ribose) polymerase 10 (PARP10) and other mono-ADP-ribosyl transferases including PARP7, PARP11, PARP12, PARP14, and PARP15. With an IC50 of 7.8 nM, OUL232 represents the most effective PARP10 inhibitor characterized to date and is the first reported inhibitor targeting PARP12. This compound is valuable for studying the biological roles of PARP10 and PARP12 in cellular processes and may facilitate research into therapeutic strategies involving these targets.

PARP/EZH2-IN-1 is a potent dual inhibitor targeting PARP and EZH2, with respective IC50 values of 6.87 nM and 36.51 nM. This reagent demonstrates significant biological activity in the treatment of triple-negative breast cancer, particularly in cells with wild-type BRCA. Its unique mechanism of action makes it a valuable tool for research into cancer biology and therapeutic development.

Palacaparib is a potent inhibitor of PARP1, demonstrating over 8000-fold selectivity for PARP1 relative to PARP2, PARP3, PARP5a, and PARP6. It functions by selectively inhibiting PARP1 and trapping it at sites of single-strand breaks (SSBs), impeding DNA repair. This compound is investigated primarily for its anti-cancer properties, particularly in research related to HRD+ breast cancer and various advanced solid tumors.

PARP-1-IN-32 is a potent inhibitor of poly(ADP-ribose) polymerase-1 (PARP-1). This compound is utilized in cancer research to investigate the mechanisms of DNA repair and cellular response to genotoxic stress. Its ability to selectively inhibit PARP-1 makes it a valuable tool for studying the role of this enzyme in tumor biology and therapeutic resistance.

L-2286 is a potent orally active inhibitor of PARP-1. This compound demonstrates significant biological activity by alleviating carotid artery remodeling, reducing oxidative stress and inflammation in spontaneously hypertensive rats, while also providing neuroprotective effects in the dorsal hippocampus. L-2286 is applicable in research focused on hypertension and its associated vascular and neurological complications.

DP-C-4 is a Cereblon-based dual-targeting PROTAC molecule designed for the concurrent degradation of epidermal growth factor receptor (EGFR) and poly (ADP-ribose) polymerase (PARP). This compound demonstrates significant biological activity by promoting the targeted destruction of these proteins, which can be crucial in cancer research and therapeutic applications. DP-C-4 may facilitate studies investigating the interplay between EGFR and PARP pathways, potentially leading to new insights in oncology and the development of innovative treatment strategies.