Catalog No.
Product Name
Application
Product Information
Citations
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PARP1 inhibitor
Niraparib R-enantiomer (MK-4827 R-enantiomer) is an excellent PARP1 inhibitor with IC50 of 2.4 nM. -
NAD+ competitive inhibitor of PARP7
RBN-2397 is a potent, accross species and orally active NAD+ competitive inhibitor of PARP7 (IC50<3 nM). -
anticancer agent
5,7,4'-Trimethoxyflavone is isolated from Kaempferia parviflora (KP) that is a famous medicinal plant from Thailand. 5,7,4'-Trimethoxyflavone induces apoptosis, as evidenced by increments of sub-G1 phase, DNA fragmentation, annexin-V/PI staining, the Bax/Bcl-xL ratio, proteolytic activation of caspase-3, and degradation of poly (ADP-ribose) polymerase (PARP) protein.5,7,4'-Trimethoxyflavone is significantly effective at inhibiting proliferation of SNU-16 human gastric cancer cells in a concentration dependent manner. -
PARP1 Degrader
iRucaparib-AP6 is a potent PROTAC compound that selectively targets PARP1 for degradation. This non-trapping degrader inhibits both the catalytic activity and scaffolding functions of PARP1, effectively disrupting its role in DNA repair pathways. iRucaparib-AP6 is useful in studying the biology of PARP1 and its implications in cancer research, particularly in understanding resistance mechanisms to PARP inhibitors. -
PROTAC PARP1 Degrader
PROTAC PARP1 Degrader functions as a targeted protein degradation agent that specifically targets PARP1 through the MDM2 E3 ligase. This compound effectively induces PARP1 cleavage and promotes apoptosis in cancer cells, making it valuable for research in cancer therapies. The structure includes the MDM2 ligand, the PARP1 ligand, and a PEG-based linker, facilitating efficient delivery and degradation of the target protein. -
PARP1 Inhibitor
PARP-1-IN-2 is a potent inhibitor of PARP1, exhibiting an IC50 value of 149 nM. This compound demonstrates significant anti-proliferative effects on the A549 human lung adenocarcinoma epithelial cell line and induces apoptosis in these cells. Its favorable ADME profile suggests high permeability across the blood-brain barrier, making it a valuable tool for research in cancer biology and therapeutic applications targeting PARP1-related pathways. -
PARP1 Inhibitor
4,4′-Secalonic acid D is a potent inhibitor of PARP1, a key enzyme in the DNA repair pathway. This compound promotes the accumulation of reactive oxygen species (ROS) and DNA damage, leading to the activation of the caspase-3/GSDME pathway, which triggers apoptosis and pyroptosis in tumor cells. 4,4′-Secalonic acid D exhibits significant anti-tumor activity, making it a valuable tool for cancer research and therapeutic investigations. -
PARP-1 Inhibitor
PARP-1-IN-3 is a potent inhibitor of PARP-1, with IC50 values of 0.25 nM for PARP-1 and 2.34 nM for PARP-2. This benzamide derivative effectively induces apoptosis and leads to G2/M phase cell cycle arrest. PARP-1-IN-3 is valuable for research applications focused on cancer mechanisms and therapeutic strategies. -
PARP-1/HDAC Inhibitor
PARP-1/HDAC-IN-1 is a dual inhibitor targeting PARP-1 and HDAC6, exhibiting IC50 values of 68.90 nM and 510 nM, respectively. This compound demonstrates significant anticancer properties, as well as anti-migration and anti-angiogenesis activities. Its applications are relevant in cancer research, particularly in studies exploring the modulation of DNA repair mechanisms and cellular signaling pathways. -
PARP Inhibitor
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. -
PARP-1 Inhibitor
CEP-6800 is a potent inhibitor of PARP-1, known for its ability to enhance the efficacy of chemotherapeutic agents. It effectively reduces poly(ADP-ribose) accumulation induced by irinotecan and temozolomide in LoVo and HT29 xenograft models. Additionally, CEP-6800 demonstrates potential in suppressing tumor growth in Calu-6. This compound is valuable for research in cancer biology and therapy development. -
PARP
PARP-1/2-IN-1 is a highly effective inhibitor of the poly(ADP-ribose) polymerases PARP-1 and PARP-2, exhibiting IC50 values of 0.51 nM and 23.11 nM, respectively. This compound plays a critical role in cancer research by targeting DNA repair mechanisms, enhancing the efficacy of chemotherapeutic agents, and potentially improving cancer treatment outcomes. It is a valuable tool for studying PARP-related cellular processes and investigating therapeutic strategies in oncology. -
PARP-1/-2 inhibitor
CEP-9722 is a selective, orally active inhibitor of PARP-1 and PARP-2, exhibiting IC50 values of 20 nM and 6 nM, respectively. This compound demonstrates significant anticancer activity, making it a valuable tool for research in cancer therapy and DNA repair mechanisms. Its ability to inhibit these critical enzymes positions CEP-9722 as an important reagent for studying cellular responses to DNA damage and tumor susceptibility to therapeutic agents. -
PARP7 Inhibitor
PARP7-IN-21 is a potent inhibitor of PARP7, demonstrating an IC50 of less than 10 nM. This compound effectively interferes with the activity of PARP7, which is involved in the regulation of cellular processes such as DNA repair and signaling pathways related to stress response. PARP7-IN-21 is valuable for research applications focused on cancer biology, neurodegenerative diseases, and other conditions associated with PARP7 dysregulation. -
CDK9/PARP Inhibitor
CDK9/PARP-IN-1 is a potent inhibitor of CDK9 and PARP1, demonstrating IC50 values of 118 nM and 107 nM, respectively. This dual inhibition results in significant antiproliferative effects across various cancer cell lines, making it a valuable tool for cancer research. CDK9/PARP-IN-1 is particularly relevant for studies investigating the therapeutic potential of targeting these pathways in oncology. -
PARP1/CDK12 Inhibitor
Antitumor agent-104 is a potent inhibitor of PARP1 and CDK12, targeting critical pathways in DNA damage repair in tumors. By inhibiting PARP1 enzymatic activity, it effectively reduces PAR protein levels, thus impairing the cellular mechanisms that protect tumor cells. This compound serves as a valuable tool in cancer research, especially in studies focused on understanding tumor biology and exploring novel therapeutic strategies. -
PARP1 Inhibitor
PARP1-IN-53 is a potent PARP1 inhibitor with an IC50 of 0.1 nM, demonstrating high selectivity over PARP2, which has an IC50 of 23 nM. This quinazolinone derivative effectively interferes with the poly(ADP-ribose) polymerase 1 enzyme, making it a valuable compound for cancer research. Its specific action on PARP1 enables detailed studies into the mechanisms of DNA repair and cell survival in oncology. -
PARP PROTAC Degrader
PROTAC PARP1 degrader-2 is a targeted protein degradation compound designed to specifically degrade PARP1. With a DC50 of less than 10 nM in MDA-MB-231 cells, it demonstrates potent efficacy in inducing degradation. Additionally, this compound inhibits cell viability in MDA-MB-436 cells with an IC50 of less than 100 nM, making it a valuable tool for research in cancer therapeutics and the mechanistic study of PARP1 function. -
PARP Inhibitor
INO-1001 mesylate is a selective inhibitor of poly (ADP-ribose) polymerase (PARP), a critical enzyme involved in DNA repair processes. It enhances the sensitivity of cancer cells to radiation therapy by disrupting DNA repair mechanisms, leading to increased necrotic cell death. This compound is of interest in cancer research, particularly in studies aimed at overcoming resistance to radiation and improving therapeutic outcomes in tumorigenesis. -
PARP-1/2 Inhibitor
CEP-8983 is a potent inhibitor of PARP-1 and PARP-2, with IC50 values of 20 nM and 6 nM, respectively. This compound effectively enhances the sensitivity of chemotherapy-resistant cell lines and subcutaneous xenograft models to the anticancer agents Temozolomide and Camptothecin. Its ability to disrupt DNA repair mechanisms makes CEP-8983 a valuable tool for cancer research, particularly in studies focusing on therapeutic resistance and combination therapies. -
PARP-1 Inhibitor
ST7710AA1 is a potent inhibitor of PARP-1, exhibiting an IC50 value of 0.07 µM. This compound demonstrates significant antiproliferative and anticancer activity, making it a valuable tool for research in oncology and cellular biology. Its ability to inhibit PARP-1 can be leveraged to explore mechanisms of cancer cell survival and the effects of DNA damage repair pathways. -
PARP-1 Inhibitor
8-Chloroquinazolin-4-ol is a potent inhibitor of the PARP-1 enzyme, exhibiting an IC50 value of 5.65 μM. This compound serves as a nicotinamide mimic and plays a significant role in research focused on DNA repair mechanisms and cancer therapies. Its ability to modulate PARP-1 activity makes it a valuable tool for exploring therapeutic strategies in various disease models. -
PARP-1 Inhibitor
Benzo[c][1,8]naphthyridin-6(5H)-one is a potent inhibitor of poly(ADP-ribose) polymerase-1 (PARP-1) and aurora kinase A, exhibiting IC50 values of 0.311 μM and 5.5 μM, respectively. This compound demonstrates low micromolar affinity for human adenosine receptors AR A1 and hA2A, with Ki values of 4.6 and 4.8 μM. Due to its mechanistic action, Benzo[c][1,8]naphthyridin-6(5H)-one is valuable for research applications targeting DNA repair pathways and cancer therapies. -
PARP-1 Inhibitor
BSI-401 is an orally active inhibitor of PARP-1, a key enzyme involved in DNA repair processes. This compound demonstrates significant anti-cancer activity, particularly in pancreatic cancer, both as a monotherapy and in combination with Oxaliplatin. BSI-401 is valuable for research into therapeutic strategies targeting DNA damage response pathways in cancer treatment. -
PARP-2 Inhibitor
UPF-1035 is a selective inhibitor of PARP-2, exhibiting an IC50 value of 0.15 μM. This compound has been shown to increase CA1 pyramidal cell loss in the hippocampus, indicating its role in neuroprotection. UPF-1035 can be utilized in research focused on neurodegenerative diseases and the mechanisms of neuronal cell survival. -
PARP1 Inhibitor
PARP1-IN-19 is a potent inhibitor of poly (ADP-ribose) polymerase 1 (PARP1), a key enzyme involved in DNA repair mechanisms. This compound exhibits significant antitumor activity, making it a valuable tool in cancer research and therapeutic development. It is primarily utilized in studies focusing on the modulation of DNA damage response pathways and the exploration of combination therapies in oncology. -
PARP Inhibitor
NU1064 dihydrochloride is a selective inhibitor of poly(ADP-ribose) polymerase (PARP), an enzyme involved in DNA repair mechanisms. This compound enhances the cytotoxic effects of DNA-methylating agents, such as MTIC, in a concentration-dependent manner. It is valuable for research in cancer biology, particularly in studies focusing on enhancing the efficacy of chemotherapeutic agents and understanding mechanisms of DNA repair inhibition. -
PARP Inhibitor
KU-0058684 is a selective PARP inhibitor, exhibiting an IC50 of 3.2 nM for PARP-1. This reagent effectively impairs DNA double strand break repair, making it a valuable tool for investigating DNA damage response mechanisms. Its application extends to studying the therapeutic potential of PARP inhibition in various cancer models. -
PARP Inhibitor
WD2000-012547 is a selective inhibitor of poly(ADP-ribose) polymerase-1 (PARP-1), demonstrating a pKi value of 8.221. This compound effectively interferes with PARP-1 activity, which plays a crucial role in DNA repair and cellular response to DNA damage. WD2000-012547 is instrumental in research applications involving cancer therapeutics, where modulation of DNA repair pathways is of significant interest. -
PARP2 Inhibitor
OUL245 is a selective inhibitor of PARP2, exhibiting an IC50 of 44 nM. It also demonstrates inhibitory activity against other PARP family members and TNKS enzymes, with IC50 values ranging from 2.9 to 8.8 μM. This compound is valuable for research into DNA repair mechanisms and the therapeutic potential of targeting PARP enzymes in various cancer models. -
PARP-1 Inhibitor
5-AIQ hydrochloride is a selective inhibitor of PARP-1, an important enzyme involved in DNA repair. This compound exhibits protective effects against ischemia-reperfusion injury in liver tissue, making it a valuable tool for studying conditions related to hepatic ischemia-reperfusion. Its applications extend to research focused on oxidative stress and cell survival mechanisms, providing insights into potential therapeutic strategies for liver protection. -
PARP1 Inhibitor
PARP1-IN-22 is a highly potent inhibitor of poly (ADP-ribose) polymerase 1 (PARP1) with an IC50 of less than 10 nM. This compound is utilized in research focused on DNA damage repair pathways and cellular responses to oxidative stress. Its ability to inhibit PARP1 makes it valuable for studies in cancer therapy and neurodegenerative diseases, where modulation of DNA repair mechanisms is crucial. -
PARP Inhibitor
A-620223 succinate is a potent inhibitor of poly(ADP-ribose) polymerase (PARP), targeting the PARP-1 enzyme with a Ki value of 8 nM and an EC50 value of 3 nM in cellular assays. Its excellent selectivity and bioavailability make it an invaluable tool for cancer research, enabling investigations into DNA repair mechanisms and potential therapeutic strategies. This compound is particularly useful in studies focused on the efficacy of PARP inhibition in various cancer models. -
PARP1 Degrader
SK-575-NEG is a PARP1 degrader designed as a methylated counterpart of SK-575, synthesized through the methylation of the amino group in piperidine-2,6-dione. It demonstrates a strong binding affinity to PARP1, with an IC50 of 2.64 nM. However, SK-575-NEG does not induce PARP1 degradation in MDA-MB-436 and Capan-1 cell lines at concentrations up to 1 μM. This compound is valuable for research focusing on the mechanistic understanding of PARP1 inhibition and degradation pathways. -
PARP14 Inhibitor
PARP14 Inhibitor 2 is a highly selective inhibitor targeting PARP14 with an IC50 value of less than 30 nM. This compound effectively inhibits the mono-ADP-ribosyltransferase activity of PARP14, thereby modulating signaling pathways associated with IFN-γ and IL-4. By reversing protumor macrophage polarization and inhibiting pro-inflammatory responses, PARP14 Inhibitor 2 holds promise for the investigation of diseases related to PARP14, including tumors, atopic dermatitis, and autoimmune disorders. -
PARP1 Inhibitor
PARP1-IN-36 is a selective inhibitor of PARP-1, characterized as a 4-carboxamido-isoindolinone derivative with a Kd value of less than 0.01 μM. This compound exhibits significant biological activity in the modulation of cellular processes associated with DNA repair, making it a valuable tool in research focused on cancer, cardiovascular diseases, nervous system injury, and inflammation. Its potent inhibition of PARP-1 serves to elucidate the role of this enzyme in various pathological contexts. -
PARP-1 Inhibitor
6(5H)-Phenanthridinone is a potent inhibitor of PARP-1, a key enzyme involved in DNA repair processes. This compound exhibits significant immunomodulatory effects and has been shown to inhibit cell proliferation. It is employed in cancer research to explore therapeutic strategies targeting DNA repair pathways and to enhance the efficacy of chemotherapeutic agents. -
PARP1/2 Inhibitor
PARP1/2-IN-3 is a potent inhibitor of PARP1 and PARP2, exhibiting IC50 values of 0.2235 nM and <0.001 nM, respectively. This compound effectively inhibits the proliferation of Capan-1 wildtype and AZD2281 or BMN673-resistant cells, with IC50 values ranging from 1.82 to 9.98 nM. Additionally, PARP1/2-IN-3 demonstrates significant antitumor efficacy in murine models, making it a valuable tool for cancer research and therapeutic development targeting PARP pathways. -
CDK-1/PARP-1 Inhibitor
UNPD139734 is a potent inhibitor of Cyclin-Dependent Kinase 1 (CDK-1) and Poly (ADP-ribose) polymerase 1 (PARP-1), forming stable complexes with both target proteins. This compound serves as a valuable lead for the structural optimization of dual-target anticancer agents, particularly in the context of breast cancer research. Its dual inhibition mechanism offers a promising avenue for investigating novel therapeutic strategies in oncology. -
PARP1/2/7 Inhibitor
PARP-1/2/7-IN-1 is a highly potent inhibitor of poly (ADP-ribose) polymerases PARP-1, PARP-2, and PARP-7, demonstrating an IC50 of less than 10 nM. This compound is valuable for research applications focused on cancer biology, DNA repair mechanisms, and cellular stress responses. Its multifunctional inhibition can aid in the exploration of therapeutic strategies targeting PARP-mediated pathways in various diseases. -
PARP1 Inhibitor
PARP1-IN-48 is a potent and selective inhibitor of poly(ADP-ribose) polymerase 1 (PARP1), exhibiting an IC50 of 3 nM against PARP1 and 170 nM against PARP2. This compound is valuable for research in oncology, virology, and metabolic disorders, facilitating investigations into the role of PARP1 in DNA repair and cellular stress responses. Its selective action makes it an essential tool for studying therapeutic pathways in cancer treatment and other disease models. -
PARP1 Inhibitor
PARP1-IN-30 is a potent, selective inhibitor of PARP1 that exhibits cytotoxic effects in tumor cells. It effectively targets cancer cells with deficiencies in the breast cancer 1 protein (BRCA1) or BRCA2, offering a valuable tool for elucidating the role of PARP1 in DNA repair and cancer biology. This compound is particularly relevant for research applications focused on targeted cancer therapies and synthetic lethality in oncology. -
PARP Inhibitor
ARTD10/PARP10-IN-2 is a potent and non-selective inhibitor of the poly(ADP-ribose) polymerases, specifically targeting ARTD10/PARP10 and ARTD1/PARP1. With IC50 values of 2.0 μM and 9.7 μM, respectively, this compound effectively modulates mono-ADP-ribosyltransferase and poly(ADP-ribose) polymerase activities. Its ability to inhibit these pathways makes ARTD10/PARP10-IN-2 valuable for research on DNA repair mechanisms and therapeutic approaches in cancer treatment. -
PARP1 Inhibitor
ZINC000081009201 is a potent inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) with an IC50 value of 1.4767 μM. This compound demonstrates significant potential for the study of triple-negative breast cancer (TNBC) by targeting PARP1-mediated repair pathways. Its inhibition may aid in elucidating the mechanisms of resistance and sensitivity in cancer treatment, making it a valuable tool for cancer research applications. -
PARP7 Inhibitor
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. -
PARP Inhibitor
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 Inhibitor
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.
