2. Signaling Pathways
  3. Cell Cycle/DNA Damage
    PI3K/Akt/mTOR
  4. DNA-PK

DNA-PK

DNA-dependent protein kinase

DNA-PK

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DNA-PK (DNA-dependent protein kinase) is a nuclear serine/threonine protein kinase composed of a large catalytic subunit (DNA-PKcs) and a heterodimeric DNA-targeting subunit Ku. DNA-PK is a major component of the nonhomologous end-joining (NHEJ) pathway of DNA double-strand breaks repair. DNA-PK specifically requires association with DNA for its kinase activity, plays important roles in the regulation of different DNA transactions, including transcription, replication and DNA repair, as well as in the maintenance of telomeres.

The assembly of DNA-PK at DSB ends serves as a platform to recruit Artemis, DNA ligase IV and other NHEJ factors that are involved in end-processing and ligation. Within the DNA-PK complex, Ku proteins confer high affinity to DSB ends, and function as early sensors. The subsequent recruitment of DNA-PKcs to DSBs via the Ku proteins triggers the activation of DNA-PKcs, a member of the phosphatidylinositol 3-kinase-related kinase (PIKK) family. Upon activation, DNA-PKcs phosphorylates a number of substrates, including H2AX, XRCC4, Artemis and most importantly, DNA-PKcs itself. Autophosphorylation of DNA-PKcs occurs at numerous Ser/Thr residues throughout the kinase, and has been shown to mediate NHEJ.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-144036
    DNA-PK-IN-3
    		Inhibitor
    DNA-PK-IN-3 is a potent inhibitor of DNA-PK. DNA-PK-IN-3 synergistically enhances the effect of radiotherapy and chemotherapy and effectively inhibits tumor growth. DNA-PK-IN-3 also effectively reduces the damage to normal cells and reducing side effects. DNA-PK-IN-3 has the potential for the research of cancer disease (extracted from patent WO2021213460A1, compound 4).
    DNA-PK-IN-3
  • HY-147567
    ATR-IN-15
    		Inhibitor
    ATR-IN-15 (compound 1) is an orally active and potent ATR kinase inhibitor, with an IC50 of 8 nM. ATR-IN-15 also inhibits human colon tumor cells LoVo, DNA-PK and PI3K, with IC50 values of 47, 663 and 5131 nM, respectively.
    ATR-IN-15
  • HY-15268
    PP487
    		Inhibitor
    PP487 is a dual inhibitor of tyrosine kinase/PI(3)Ks with IC50 values of 0.017 μM, 0.072 μM, 0.004 μM, 0.01 μM, 0.55 μM, 0.22 μM, and < 0.01 μM against DNA-PK, mTOR, Hck, Src, EGFR, EphB4, and PDGFR, respectively. PP487 can be used for cancer research.
    PP487
  • HY-142943
    DNA-PK-IN-1
    		Inhibitor
    DNA-PK-IN-1 is a potent inhibitor of DNA-PK. DNA-dependent protein kinase (DNA-PK) is a DNA-PK enzyme complex composed of Ku70/Ku80 heterodimer and DNA-dependent protein kinase catalytic subunit (DNA-PKcs). DNA-PK-IN-1 has the potential for the research of cancer diseases (extracted from patent WO2021136463A1, compound 1).
    DNA-PK-IN-1
  • HY-146566
    DNA-PK-IN-9
    		Inhibitor
    DNA-PK-IN-9 (compound YK6) is a potent DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 value of 10.47 nM. DNA-PK-IN-9 can be used for researching anticancer.
    DNA-PK-IN-9
  • HY-142471
    ZL-2201 free base
    		Inhibitor
    ZL-2201 free base is a potent DNA-PK inhibitor with an IC50 of 1 nM (WO2021104277A1, compound 5).
    ZL-2201 free base
  • HY-162692
    DNA-PK-IN-14
    		Inhibitor
    DNA-PK-IN-14 (compound 78) is a potent, selective DNA-PK inhibitor with an IC50 value of 7.95 nM. DNA-PK-IN-14 has oral activity and has the potential to be a radiosensitizer for cancer treatment.
    DNA-PK-IN-14
  • HY-144037
    DNA-PK-IN-4
    		Inhibitor
    DNA-PK-IN-4 is a potent inhibitor of DNA-PK. DNA-PK-IN-4 is a imidazolinone derivative compound. DNA-PK-IN-4 inhibits DNA-PKcs activity, thus greatly reducing tumor DNA repair and inducing cells to enter the apoptotic program. DNA-PK-IN-4 has the potential for the research of cancer disease (extracted from patent WO2021209055A1, compound 27).
    DNA-PK-IN-4
  • HY-153943
    DNA-PK-IN-10
    		Inhibitor
    DNA-PK-IN-10 is a DNA-PK inhibitor. DNA-PK-IN-10 can be used for the research of breast cancer and non-small cell lung cancer.
    DNA-PK-IN-10
  • HY-158166
    DNA-PK-IN-13
    		Inhibitor
    DNA-PK-IN-13 (Compound SK10) is a DNA-PK inhibitor that exhibits potent inhibitory activity (IC50= 0.11 nM). DNA-PK-IN-13 regulates tumor cell proliferation by decreasing the expression level of γH2A.X and enhancing the sensitivity of tumor cells to chemotherapeutic agents. DNA-PK-IN-13 is suitable for oncology studies.
    DNA-PK-IN-13
  • HY-144039
    DNA-PK-IN-6
    		Inhibitor
    DNA-PK-IN-6 is a potent inhibitor of DNA-PK. DNA-PK-IN-6 inhibits DNA-PKcs activity, thus greatly reducing tumor DNA repair and inducing cells to enter the apoptotic program. DNA-PK-IN-6 enhances the sensitivity of tumor tissues to radiotherapy, overcomes the problem of agent resistance, and enhances the inhibitory effect on a variety of solid tumors and hematological tumors (extracted from patent WO2021197159A1, compound 6).
    DNA-PK-IN-6
Cat. No. Product Name / Synonyms Application Reactivity