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DNA-dependent protein kinase (DNA-PK) inhibitors block a central enzyme in the repair of DNA double-strand breaks. DNA-PK consists of a large catalytic subunit (DNA-PKcs) and the Ku70/Ku80 heterodimer, which binds broken DNA ends. A 1993 study showed that the kinase requires DNA ends for activity and associates with the Ku antigen. Active DNA-PK drives non-homologous end joining, the main pathway that rejoins double-strand breaks without a template. NU-7441, identified in 2004 by screening chromenone libraries, and NU7026 are DNA-PK-selective tools. DNA-PKcs is related to phosphoinositide 3-kinases (PI3Ks), so PI-103 and CC-115 also inhibit PI3K or mammalian target of rapamycin (mTOR).
ZL-2201 is a potent inhibitor of DNA-dependent protein kinase (DNA-PK) with an IC50 value of 1 nM. This compound plays a critical role in the study of DNA repair mechanisms and cellular responses to DNA damage. It is valuable for researchers investigating cancer biology, therapeutic resistance, and the modulation of DNA repair pathways.
DNA-PK-IN-8 is a selective and potent inhibitor of DNA-dependent protein kinase (DNA-PK) with an IC50 value of 0.8 nM. This compound displays synergistic antiproliferative effects on various cancer cell lines and significantly reduces HL-60 tumor growth when used in combination with Doxorubicin. DNA-PK-IN-8 is an invaluable tool for studying DNA repair mechanisms and exploring therapeutic strategies in oncology research.
Synonyms: (R)-M9831
(R)-VX-984 is the (R)-enantiomer of VX-984, a potent inhibitor of DNA-dependent protein kinase (DNA-PK). This compound effectively impairs DNA repair mechanisms, making it a valuable tool for elucidating the role of DNA-PK in cellular processes. Its inhibitory action positions (R)-VX-984 as a significant reagent for research in cancer biology and therapeutic interventions targeting DNA repair pathways.
NU5455 is a selective and potent inhibitor of DNA-dependent protein kinase catalytic subunit (DNA-PKcs). This compound significantly enhances the efficacy and toxicity of parenterally administered topoisomerase inhibitors, particularly Doxorubicin, in liver tumor xenografts, while maintaining a favorable safety profile. NU5455 is valuable in cancer research, specifically in studies focused on DNA repair mechanisms and therapeutic strategies for optimizing chemotherapeutic outcomes.
DNA-PK-IN-15 is a potent inhibitor of DNA-dependent protein kinase (DNA-PK) with an IC50 of 0.08 nM. This compound effectively hinders DNA repair mechanisms, making it a valuable tool for studying the cellular responses to DNA damage and the effects of DNA-PK modulation in various biological contexts. Research applications include cancer therapy development and understanding the role of DNA-PK in genomic stability.
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DNA-PK-IN-2 is a potent inhibitor of DNA-dependent protein kinase (DNA-PK), a critical enzyme complex involved in DNA repair, consisting of Ku70/Ku80 heterodimer and DNA-PK catalytic subunit (DNA-PKcs). This compound is designed for research applications focused on cancer biology, where modulation of DNA repair pathways is essential. DNA-PK-IN-2 may provide insights into cancer treatment strategies by disrupting DNA repair mechanisms in tumor cells.
DNA-PK-IN-5 is a potent inhibitor of DNA-dependent protein kinase (DNA-PK), specifically targeting the catalytic subunit DNA-PKcs. This compound effectively disrupts tumor DNA repair mechanisms, promoting apoptosis in cancer cells. DNA-PK-IN-5 has been shown to enhance the sensitivity of tumor tissues to radiotherapy and addresses challenges related to agent resistance, providing a robust inhibitory effect on various solid tumors and hematological malignancies.
SU-11752 is a potent inhibitor of DNA-dependent protein kinase (DNA-PK), exhibiting an IC50 value of 0.13 μM. This compound also inhibits the PI3K p110γ kinase with an IC50 of 1.1 μM. By competitively binding to the ATP-site of DNA-PK, SU-11752 effectively disrupts intracellular DNA double-strand break repair mechanisms, thereby enhancing the sensitivity of cells to radiotherapy. This makes it a valuable tool in cancer research and therapy applications.
DNA-PK-IN-3 is a selective inhibitor of DNA-dependent protein kinase (DNA-PK), an essential component of DNA repair mechanisms. This compound enhances the efficacy of radiotherapy and chemotherapy while effectively inhibiting tumor growth. Additionally, DNA-PK-IN-3 has been shown to minimize damage to normal cells, thereby reducing associated side effects. Its potential applications extend to cancer research, providing valuable insights into therapeutic strategies targeting DNA repair pathways.
DNA-PK-IN-1 is a potent inhibitor of DNA-dependent protein kinase (DNA-PK), a key enzyme complex comprised of the Ku70/Ku80 heterodimer and the DNA-PK catalytic subunit (DNA-PKcs). This compound exhibits significant activity in inhibiting DNA-PK, making it a valuable tool for investigating DNA damage response and repair mechanisms in cancer research. Its application is particularly relevant in studies aimed at understanding tumor biology and developing targeted cancer therapies.
ZL-2201 free base is a highly selective inhibitor of DNA-dependent protein kinase (DNA-PK), demonstrating an IC50 of 1 nM. This compound has significant implications in research applications focused on DNA repair mechanisms, cancer therapy, and radiation sensitization. ZL-2201 is ideal for studies investigating the modulation of DNA damage response pathways.
DNA-PK-IN-14 is a potent selective inhibitor of DNA-dependent protein kinase (DNA-PK) with an IC50 value of 7.95 nM. This compound exhibits oral bioactivity and demonstrates potential as a radiosensitizer in cancer treatment. It can be utilized in research applications focusing on DNA repair mechanisms and the enhancement of radiotherapy efficacy.
DNA-PK-IN-4 is a potent inhibitor of DNA-dependent protein kinase (DNA-PK), specifically targeting DNA-PKcs activity. As an imidazolinone derivative, it effectively diminishes DNA repair capabilities in tumor cells, leading to increased apoptosis. This compound is valuable for research applications focused on cancer biology and the exploration of therapeutic strategies targeting DNA repair pathways.
DNA-PK-IN-10 is a selective inhibitor of DNA-dependent protein kinase (DNA-PK), a critical enzyme involved in the DNA damage response and repair mechanisms. This compound has demonstrated significant potential in the investigation of tumorigenesis, particularly in breast cancer and non-small cell lung cancer models. Its application in research may aid in understanding the roles of DNA-PK in cancer cell survival and resistance to therapies, providing insights for the development of targeted treatments.
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IC-87361 is a selective inhibitor of DNA-dependent protein kinase catalytic subunit (DNA-PKcs), serving as a potent radiosensitizer. By inhibiting the catalytic activity of DNA-PKcs, IC-87361 effectively disrupts non-homologous end joining (NHEJ) pathways involved in the repair of DNA double-strand breaks. This compound is particularly valuable in research related to lung cancer and melanoma, providing insights into therapeutic strategies that target DNA repair mechanisms.
DNA-PK-IN-6 is a selective inhibitor of DNA-dependent protein kinase (DNA-PK), specifically targeting DNA-PKcs activity. By inhibiting this kinase, DNA-PK-IN-6 significantly reduces the DNA repair capacity of tumor cells, thereby promoting apoptosis. This compound enhances the sensitivity of various solid tumors and hematological malignancies to radiotherapy, addressing challenges related to treatment resistance. Its applications are crucial for research in cancer therapeutics and treatment strategies.
OK-1035 is a selective inhibitor of DNA-dependent protein kinase (DNA-PK), exhibiting an IC50 value of 100 μM. It interferes with DNA double strand break repair mechanisms, thus providing valuable insights into cellular responses to DNA damage. This compound has potential applications in cancer research, particularly in studies focused on enhancing the efficacy of radiotherapy and chemotherapeutics.
NU-7163 is an ATP-competitive inhibitor of DNA-dependent protein kinase (DNA-PK), demonstrating an IC50 of 0.19 μM and a Ki of 24 nM. This compound enhances the cytotoxic effects of ionizing radiation in the HeLa human tumor cell line, making it a valuable tool for research in cancer biology and therapeutic development. NU-7163 may be particularly relevant in studies exploring DNA repair mechanisms and enhancing the effectiveness of radiotherapy.
