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-10108
    LY294002
    		Inhibitor 99.95%
    LY294002 is a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively. LY294002 also inhibits CK2 with an IC50 of 98 nM. LY294002 is a competitive DNA-PK inhibitor that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4?μM. LY294002 is an apoptosis activator.
    LY294002
  • HY-111783
    AZD-7648
    		Inhibitor 99.86%
    AZD-7648 is a potent, orally active, selective DNA-PK inhibitor with an IC50 of 0.6 nM. AZD-7648 induces apoptosis and shows antitumor activity.
    AZD-7648
  • HY-11006
    KU-57788
    		Inhibitor 99.95%
    KU-57788 (NU7441) is a highly potent and selective DNA-PK inhibitor with an IC50 of 14 nM. KU-57788 is an NHEJ pathway inhibitor. KU-57788 also inhibits PI3K and mTOR with IC50s of 5.0 and 1.7 μM, respectively.
    KU-57788
  • HY-13002
    Torin 2
    		Inhibitor 99.65%
    Torin 2 is an mTOR inhibitor with EC50 of 0.25 nM for inhibiting cellular mTOR activity, and exhibits 800-fold selectivity over PI3K (EC50: 200 nM). Torin 2 also inhibits DNA-PK with an IC50 of 0.5 nM in the cell free assay. Torin 2 can suppress both mTORC1 and mTORC2.
    Torin 2
  • HY-101570
    Nedisertib
    		Inhibitor 99.70%
    Nedisertib (M3814) is a potent, orally available and selective inhibitor of DNA-PK, with an IC50 of <3 nM. Anti-tumor activity.
    Nedisertib
  • HY-169248
    DNA-PK-IN-15
    		Inhibitor
    DNA-PK-IN-15 (compound 6) is an inhibitor of DNA-PK with an IC50 value of 0.08 nM.
    DNA-PK-IN-15
  • HY-114923
    SU-11752
    		Inhibitor
    SU-11752 is an inhibitor for DNA-dependent protein kinase (DNA-PK) with an IC50 of 0.13 μM. SU-11752 inhibits PI3K p110γ kinase with IC50 of 1.1 μM. SU-11752 binds competitively for ATP-site in DNA-PK, results in inhibition of intracellular DNA double-strand break repair and increases the sensitivity of cells to radiotherapy.
    SU-11752
  • 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-10115
    PI-103
    		Inhibitor 98.93%
    PI-103 is a potent PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 also inhibits DNA-PK with an IC50 of 2 nM. PI-103 induces autophagy.
    PI-103
  • HY-122727
    STL127705
    		Inhibitor ≥98.0%
    STL127705 (Compound L) is a potent Ku 70/80 heterodimer protein inhibitor with an IC50 of 3.5 μM. STL127705 interferes the binding of Ku70/80 to DNA and by inhibits the activation of the DNA-PKCS kinase. STL127705 shows antiproliferative and anticancer activity. STL127705 induces apoptosis.
    STL127705
  • HY-15719
    NU 7026
    		Inhibitor 99.86%
    NU 7026 (LY293646) is a novel specific DNA-PK inhibitor with IC50 of 0.23 μM, also inhibits PI3K with IC50 of 13 μM.
    NU 7026
  • HY-12513
    Samotolisib
    		Inhibitor 99.27%
    Samotolisib (LY3023414) potently and selectively inhibits class I PI3K isoforms, DNA-PK, and mTORC1/2 with IC50s of 6.07 nM, 77.6 nM, 38 nM, 23.8 nM, 4.24 nM and 165 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, DNA-PK and mTOR, respectively. Samotolisib potently inhibits mTORC1/2 at low nanomolar concentrations.
    Samotolisib
  • HY-12030
    PIK-90
    		Inhibitor 99.70%
    PIK-90 is a DNA-PK and PI3K inhibitor, which inhibits p110α, p110γ and DNA-PK with IC50s of 11, 18 and 13 nM, respectively.
    PIK-90
  • HY-13281
    PIK-75 hydrochloride
    		Inhibitor 99.72%
    PIK-75 hydrochloride 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 hydrochloride inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM). PIK-75 hydrochloride induces apoptosis.
    PIK-75 hydrochloride
  • HY-16962
    CC-115
    		Inhibitor 99.82%
    CC-115 is a potent and dual DNA-PK and mTOR kinase inhibitor with IC50s of 13 nM and 21 nM, respectively. CC-115 blocks both mTORC1 and mTORC2 signaling.
    CC-115
  • HY-19939S
    VX-984
    		Inhibitor 98.86%
    VX-984 is an orally active, potent, selective and BBB-penetrated DNA-PK inhibitor. VX-984 efficiently inhibits NHEJ (non-homologous end joining) and increases DSBs (DNA double-strand breaks). VX-984 can be used for glioblastomas (GBM) and non-small cell lung cancer (NSCLC) research. VX-984 is a de novo deuterium.
    VX-984
  • HY-13431
    KU-0060648
    		Inhibitor 99.62%
    KU-0060648 is a dual inhibitor of PI3K and DNA-PK with IC50s of 4 nM, 0.5 nM, 0.1 nM, 0.594 nM and 8.6 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and DNA-PK, respectively.
    KU-0060648
  • HY-132293
    BAY-8400
    		Inhibitor 99.38%
    BAY-8400 is an orally active, potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (IC50=81 nM). BAY-8400 can be used for the research of cancer.
    BAY-8400
  • HY-10115A
    PI-103 Hydrochloride
    		Inhibitor 98.00%
    PI-103 Hydrochloride is a dual PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 Hydrochloride also inhibits DNA-PK with an IC50 of 2 nM. PI-103 Hydrochloride induces autophagy.
    PI-103 Hydrochloride
  • HY-16962A
    CC-115 hydrochloride
    		Inhibitor 98.03%
    CC-115 hydrochloride is a potent and dual DNA-PK and mTOR kinase inhibitor with IC50s of 13 nM and 21 nM, respectively. CC-115 blocks both mTORC1 and mTORC2 signaling.
    CC-115 hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity