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-163134
    DNA-PK-IN-12
    		Inhibitor
    DNA-PK-IN-12 (compound 31t) is an oral active DNA-PK inhibitor with the IC50 of 0.1 nM. DNA-PK-IN-12 inhibits cell growth and Hct116 cell colony formation with the IC50 of 33.28 μM, and shows antitumor activity in vivo.
    DNA-PK-IN-12
  • 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-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-107834
    PIK-75
    		Inhibitor 98.72%
    PIK-75 is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM). PIK-75 induces apoptosis.
    PIK-75
  • HY-160096
    DNA-PK-IN-11
    		Inhibitor 99.10%
    DNA-PK-IN-11 is a DNA-PK inhibitor with an IC50 of <0.1 μM (DE102010035744A1; compound 36).
    DNA-PK-IN-11
  • 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