Catalog No.
Product Name
Application
Product Information
Citations
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PI3K Inhibitor
PI-103 is a potent, cell-permeable, ATP-competitive inhibitor of phosphatidylinositol 3-kinase (PI3K) family members with selectivity toward DNA-PK, PI3K (p110α), and mTOR.- Diane Yang, .et al. , Diabetes, 2021, Oct;70(10):2419-2429 PMID: 34344789
- Byungki Jang, .et al. , Int J Mol Sci, 2017, Nov; 18(11): 2258 PMID: 29077055
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PI3K Inhibitor
PIK-75 is an imidazopyridine that selectively inhibits p110α with an IC50 value of 5.8 nM.2 It inhibits p110γ and p110β considerably less effectively with IC50 values of 0.076 μM and 1.3 μM, respectively.- Pridham KJ, .et al. , Neuro Oncol, 2018, Mar 27;20(4):494-505 PMID: 29016844
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DNA-PK inhibitor
NU-7441 (KU-57788) is a potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor. The IC50 values are 14, 1700, 5000, >100000 and >100000 nM for DNA-PK, mTOR, PI 3-K, ATM and ATR respectively.- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Ryo Sakasai, .et al. , Biochem Biophys Res Commun, 2023, Aug 6;668:42-48 PMID: 37244033
- Shahar Biechonski, .et al. , Sci Rep, 2018, Apr 17 PMID: 29666389
- Ihara M, .et al. , J Radiat Res, 2018, Nov 23 PMID: 30476230
- Chwastek J, .et al. , Int J Biochem Cell Biol, 2017, Jun;87:38-53 PMID: 28341201
- Masaaki Yanai, .et al. , Yonago Acta Med, 2017, Mar; 60(1): 9-15 PMID: 28331416
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DNA-PK inhibitor
Compound 401 is a cell-permeable pyrimido-isoquinolinone compound that acts as a potent, reversible, and ATP-competitive inhibitor of DNA-PK (IC50 = 280 nM) with ~19-fold selectivity over mTOR (IC50 = 5.3 μM). -
DNA-PK inhibitor
NU7026 is a novel DNA-dependent protein kinase inhibitor that potentiates the cytotoxicity of topoisomerase II poisons used in the treatment of leukemia.- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Velichko AK, .et al. , Nucleic Acids Res, 2019, May 22. pii: gkz436 PMID: 31114877
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DNA-PK inhibitor
KU0060648 is a potent and selective inhibitor of DNA-dependent protein kinase (DNA-PK), (IC50 = 8.6 nM); with 20-1000 fold selectivity for DNA-PK over other PIKKs and a panel of 60 kinases. KU-0060648 enhances HDR efficiency and attenuates NHEJ frequency. -
ATR inhibitor
ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM.- Fu-Xing Gong, .et al. , Nucleic Acids Res, 2021, Sep 20;49(16):9342-9352 PMID: 34403458
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DNA-PK inhibitor
Nedisertib, also known as M-3814, MSC2490484A, is an orally available inhibitor of DNA-dependent protein kinase (DNA-PK), with potential antineoplastic and chemo/radiosensitizing activities. - (R)-Nedisertib ((R)-M3814) is a less active R-enantiomer of Nedisertib, with an IC50 in the range of 7-30 nM for DNA-PK.
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DNA-PK inhibitor
(Rac)-Nedisertib ((Rac)-M3814) is a racemate of Nedisertib, a potent DNA-PK inhibitor, with an IC50 of <3 nM. -
DNA-PK Inhibitor
IC 86621 is a potent inhibitor of DNA-dependent protein kinase (DNA-PK) with an IC50 of 120 nM, acting as a selective and reversible ATP-competitive inhibitor. This compound impedes DNA-PK mediated repair of DNA double-strand breaks (DSB), displaying an EC50 of 68 µM. IC 86621 enhances antitumor activity in the presence of DSBs without inducing cytotoxicity and provides protection against apoptosis in T cells from rheumatoid arthritis. Its applications extend to cancer research and the study of immune responses in autoimmune disorders. -
DNA-PK/p110α Inhibitor
PIK-75 is a selective inhibitor of DNA-PK and p110α, exhibiting IC50 values of 2 nM and 5.8 nM, respectively, while demonstrating over 200-fold greater potency against p110α compared to p110β (IC50 = 1.3 μM). This compound effectively induces apoptosis, making it a valuable tool for research in cancer biology and therapies targeting DNA repair pathways. Its specificity for these kinases facilitates investigations into their roles in cellular processes and potential therapeutic interventions. -
ATM/ DNA-PKcs Inhibitor
XRD-0394 is a highly potent and orally active inhibitor of ATM and DNA-PKcs, exhibiting IC50 values of 0.39 nM and 0.89 nM, respectively. This compound demonstrates selectivity for its target enzymes over other members of the PIKK and PI3K families. In preclinical studies, XRD-0394 has been shown to significantly enhance the cytotoxic effects of ionizing radiation on tumor cells both in vitro and in vivo. Additionally, it can synergize with PARP and topoisomerase I inhibitors, making it a valuable tool for research in cancer treatment and DNA repair mechanisms. -
DNA-PK Inhibitor
NU-7031 is a coumarin derivative that selectively inhibits DNA-PK with an IC50 of 1.7 μM. This compound is utilized in cancer research to investigate DNA repair mechanisms and therapeutic strategies targeting DNA damage response pathways. Its role as a DNA-PK inhibitor makes it a valuable tool for understanding the implications of DNA repair in tumor biology. -
DNA-PK/mTOR Inhibitor
CC-115 hydrochloride is a potent dual inhibitor of DNA-PK and mTOR, exhibiting IC50 values of 13 nM and 21 nM, respectively. It effectively disrupts signaling pathways associated with both mTORC1 and mTORC2. This compound is valuable for research focused on cancer therapeutics and the modulation of DNA damage response mechanisms. -
DNA-PK Inhibitor
VX-984 is a potent and selective DNA-PK inhibitor that effectively penetrates the blood-brain barrier. It disrupts the non-homologous end joining (NHEJ) repair pathway, leading to an increase in DNA double-strand breaks (DSBs). This compound has significant research applications in the study of glioblastomas (GBM) and non-small cell lung cancer (NSCLC). Ideal for investigations into cancer therapy and DNA damage response mechanisms. -
DNA-PK Inhibitor
BAY-8400 is a potent and selective inhibitor of DNA-dependent protein kinase (DNA-PK), with an IC50 of 81 nM. This orally active compound is primarily employed in cancer research, where it can help elucidate DNA repair mechanisms and investigate therapeutic strategies targeting DNA damage response pathways. -
DNA-PK Inhibitor
DNA-PK-IN-12 is a potent DNA-PK inhibitor, displaying an IC50 of 0.1 nM. This compound effectively inhibits cell growth and Hct116 cell colony formation with an IC50 of 33.28 μM. Additionally, DNA-PK-IN-12 demonstrates significant antitumor activity in vivo, making it a valuable reagent for cancer research and therapeutic studies. -
DNA-PK Inhibitor
AMA-37 is an ATP-competitive inhibitor of DNA-dependent protein kinase (DNA-PK), demonstrating an IC50 value of 0.27 μM for this target. In addition, it shows moderate inhibitory activity against phosphoinositide 3-kinase isoforms with IC50 values of 32 μM for p110α, 3.7 μM for p110β, and 22 μM for p110γ. This compound is suitable for research applications focusing on DNA repair mechanisms and cancer therapeutics, where modulation of DNA-PK activity may be beneficial. -
DNA-PK Inhibitor
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 Inhibitor
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. -
DNA-PK Inhibitor
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 Inhibitor
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. -
DNA-PK Inhibitor
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 Inhibitor
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. -
DNA-PK Inhibitor
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 Inhibitor
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 Inhibitor
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. -
DNA-PK Inhibitor
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 inhibitor
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 Inhibitor
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 Inhibitor
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. -
DNA-PKcs Inhibitor
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 Inhibitor
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. -
DNA-PK Inhibitor
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. -
DNA-PK Inhibitor
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.
