PARP

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.

Items 101-125 of 236

  • PARP1-IN-6
    Cat. No.
    A29001

    PARP1-IN-6

    PARP1-IN-6 is a dual inhibitor of tubulin and PARP-1, displaying IC50 values of 0.94 μM and 0.48 μM, respectively. This compound demonstrates significant biological activity by disrupting cellular processes mediated by both targets, making it a valuable tool for cancer research. PARP1-IN-6 is particularly useful in studies investigating the roles of PARP inhibition in DNA repair mechanisms and cytoskeletal dynamics.

    5 mg
    $795.00
    All 1 sizes
  • DPQ hydrochloride
    Cat. No.
    A29002

    DPQ hydrochloride

    Synonyms: 6,7-Dimethoxy-2-(1-piperazinyl)-4-quinazolinamine hydrochloride

    DPQ hydrochloride is a potent and selective inhibitor of PARP-1 (poly(ADP-ribose) polymerase 1), effectively blocking PARP-1-mediated DNA damage repair and reducing NAD+/ATP consumption. This compound demonstrates significant anti-inflammatory properties by inhibiting the activation of the NF-κB pathway, leading to a decrease in pro-inflammatory cytokines such as TNF-α and IL-6, as well as mitigating oxidative stress. DPQ hydrochloride is ideal for research applications related to inflammation and can be utilized in studies of conditions such as acute lung injury, myocardial infarction, and neurodegenerative diseases.

    1 mg
    $55.00
    5 mg
    $130.00
    All 6 sizes
  • Lotixparib
    Cat. No.
    A29003

    Lotixparib

    Lotixparib is a potent inhibitor of poly(ADP-ribose) polymerase-1 (PARP-1), a key enzyme involved in DNA damage repair. This compound demonstrates cytoprotective effects, offering potential therapeutic applications in retinal diseases. Lotixparib is valuable for research focused on PARP-1-related conditions and mechanisms underlying DNA repair pathways.

    Out of stock

    All 3 sizes
  • PARP7-IN-23
    Cat. No.
    A29006

    PARP7-IN-23

    PARP7-IN-23 is a potent inhibitor of Poly(ADP-ribose) polymerase 7 (PARP7) with an EC50 of 0.915 nM for phosphorylated STAT1 (pSTAT1) in NCI-H1373 cells. This compound demonstrates significant inhibitory activity, which positions it as a valuable tool for cancer research, particularly in studies involving STAT1 signaling pathways and therapeutic interventions targeting PARP7.

    Out of stock

    All 3 sizes
  • PARP1-IN-21
    Cat. No.
    A29007

    PARP1-IN-21

    PARP1-IN-21 is a potent inhibitor of PARP1, exhibiting an IC50 of less than 10 nM. This compound effectively disrupts the poly(ADP-ribose) polymerase 1 enzymatic activity, leading to the inhibition of DNA repair processes. It is primarily utilized in research applications focused on cancer biology and therapeutic development, particularly in the exploration of combination therapies for tumors with defective homologous recombination.

    25 mg
    $1,655.00
    50 mg
    $2,115.00
    All 3 sizes
  • PARP1-IN-43
    Cat. No.
    A29010

    PARP1-IN-43

    PARP1-IN-43 is a potent PARP1 inhibitor with an IC50 of 5 nM, exhibiting effective penetration across the blood-brain barrier. This compound is primarily utilized in research focused on homologous recombination-deficient central nervous system (CNS) tumors, facilitating the exploration of targeted therapies in oncology. Its ability to selectively inhibit PARP1 makes it a valuable reagent for investigating DNA repair mechanisms and their implications in cancer biology.

    Out of stock

    All 3 sizes
  • PARP1-IN-39
    Cat. No.
    A29011

    PARP1-IN-39

    PARP1-IN-39 is a potent inhibitor of PARP1, exhibiting an IC50 of 0.22 nM, and an IC50 of 1.57 nM in human breast cancer cells. This compound is valuable for investigating cancers associated with DNA repair deficiencies, including those linked to BRCA1/2 mutations, and is applicable in studies of breast, ovarian, pancreatic, and prostate cancers. PARP1-IN-39 facilitates research into targeted therapies that exploit the vulnerabilities of cancer cells with defective DNA repair mechanisms.

    Out of stock

    All 3 sizes
  • TNKS 22
    Cat. No.
    A29012

    TNKS 22

    Synonyms: TNKS-IN-22

    TNKS 22 is a selective inhibitor of tankyrase 1 and tankyrase 2. It demonstrates potent inhibitory activity, with IC50 values of 0.1 nM and 4.1 nM for TNKS1 and TNKS2, respectively. This compound serves as a valuable tool for research into the roles of tankyrases in cellular processes such as the Wnt signaling pathway and telomere regulation. Applications include studies in cancer biology and therapeutic development targeting poly(ADP-ribose) polymerase pathways.

    Out of stock

    All 3 sizes
  • KCL-440
    Cat. No.
    A29014

    KCL-440

    KCL-440 is a potent PARP inhibitor that effectively penetrates the central nervous system, exhibiting an IC50 of 68 nM for PARP-1 inhibition. This compound is primarily utilized in research exploring DNA repair mechanisms, cancer therapy, and neurodegenerative disease models, making it a valuable tool for studying therapeutic strategies targeting cellular stress responses.

    25 mg
    $1,655.00
    50 mg
    $2,115.00
    All 3 sizes
  • TIPARP-IN-1
    Cat. No.
    A29016

    TIPARP-IN-1

    TIPARP-IN-1 is a selective inhibitor of PARP7 (TIPARP) with an IC50 of 2.15 nM. By inhibiting TIPARP, this compound restores the interferon signaling pathway in tumors, effectively enhancing the anti-tumor immune response within the tumor microenvironment while minimizing systemic cytokine production. TIPARP-IN-1 is an important tool for investigating the role of PARP7 in head and neck squamous cell carcinoma.

    Out of stock

    All 3 sizes
  • 4-Aminonaphthalimide
    Cat. No.
    A29017

    4-Aminonaphthalimide

    4-Aminonaphthalimide is a potent inhibitor of poly(ADP-ribose) polymerase (PARP), a key enzyme involved in DNA repair processes. This compound enhances the cytotoxic effects of γ-radiation in cancer cells, making it a valuable tool for studies focused on cancer therapy and radiation biology. Its dual function as a PARP inhibitor and radiation sensitizer positions 4-Aminonaphthalimide as an important reagent for research applications in oncology and therapeutic resistance.

    5 mg
    $25.00
    10 mg
    $40.00
    All 6 sizes
  • PARP1-IN-51
    Cat. No.
    A29018

    PARP1-IN-51

    PARP1-IN-51 is a potent inhibitor of the enzyme PARP1, which plays a critical role in DNA repair mechanisms. This compound exhibits significant biological activity by disrupting the PARP1-mediated repair of single-strand breaks, ultimately leading to cancer cell apoptosis. PARP1-IN-51 is particularly valuable for research in oncology, including studies focused on breast cancer and other malignancies with defective DNA repair pathways.

    Out of stock

    All 3 sizes
  • PARP1-IN-37
    Cat. No.
    A29019

    PARP1-IN-37

    PARP1-IN-37 is a selective inhibitor of poly(ADP-ribose) polymerases 1 and 2 (PARP1/2), exhibiting an IC50 of 24 nM for PARP1. This compound effectively inhibits PARP activity in cellular assays with an EC50 of 3.7 μM. PARP1-IN-37 is particularly relevant for investigations into BRCA-mutated tumors, including breast and ovarian cancers, making it a valuable tool for cancer research and therapeutic development.

    Out of stock

    All 3 sizes
  • Tankyrase-IN-3
    Cat. No.
    A29020

    Tankyrase-IN-3

    Tankyrase-IN-3 is a selective inhibitor of tankyrase 1 (TNKS1), demonstrating an IC50 value of 22 nM. This compound plays a significant role in the regulation of Wnt signaling pathways and cellular processes related to tumorigenesis. Tankyrase-IN-3 is primarily utilized in cancer research, offering insights into the therapeutic mechanisms targeting TNKS1 in various malignancies.

    Out of stock

    All 3 sizes
  • PARP1-IN-18
    Cat. No.
    A29021

    PARP1-IN-18

    PARP1-IN-18 is a potent inhibitor of the poly(ADP-ribose) polymerase 1 (PARP1) enzyme, demonstrating an IC50 value of 2.7 nM. This compound exhibits significant anticancer activity, making it a valuable tool for research applications targeting DNA repair mechanisms and cancer therapeutics. PARP1-IN-18 can be utilized to explore PARP-mediated cellular processes and evaluate its potential in combination therapies for various malignancies.

    Out of stock

    All 3 sizes
  • PARP7-IN-24
    Cat. No.
    A29022

    PARP7-IN-24

    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.

    Out of stock

    All 3 sizes
  • PARP-1-IN-23
    Cat. No.
    A29024

    PARP-1-IN-23

    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.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • Senaparib hydrochloride
    Cat. No.
    A29026

    Senaparib hydrochloride

    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.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • PARP-2/1-IN-2
    Cat. No.
    A29027

    PARP-2/1-IN-2

    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.

    5 mg
    $200.00
    10 mg
    $325.00
    All 5 sizes
  • PARP1-IN-28
    Cat. No.
    A29028

    PARP1-IN-28

    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.

    Out of stock

    All 3 sizes
  • PARP1/2-IN-4
    Cat. No.
    A29030

    PARP1/2-IN-4

    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.

    Out of stock

    All 3 sizes
  • PARP10-IN-2
    Cat. No.
    A29032

    PARP10-IN-2

    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.

    5 mg
    $20.00
    10 mg
    $35.00
    All 6 sizes
  • KMR-206
    Cat. No.
    A29033

    KMR-206

    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.

    1 mg
    $185.00
    5 mg
    $400.00
    All 4 sizes
  • YCH1899
    Cat. No.
    A29034

    YCH1899

    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.

    5 mg
    $165.00
    10 mg
    $275.00
    All 4 sizes
  • PARP1-IN-29
    Cat. No.
    A29035

    PARP1-IN-29

    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.

    1 mg
    $520.00
    5 mg
    $1,225.00
    All 5 sizes

Items 101-125 of 236

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