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

DNA-PK

DNA-PK

Related Products

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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.

DNA-PK Related Products (56):

Cat. No. Product Name Effect Purity
  • 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[1].
  • 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[1][2][3].
  • HY-10108
    LY294002 Inhibitor
    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[1]. LY294002 also inhibits CK2 with an IC50 of 98 nM[2]. 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[3].
  • 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[1].
  • 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.
  • HY-172771
    Multi-target kinase inhibitor 4 Inhibitor
    Multi-target kinase inhibitor 4 (Compound 2) is a PI3K/DNA-PK inhibitor and potent chemosensitizer that can increase the amount of DNA double strand breaks induced by Doxorubicin (HY-15142A). Multi-target kinase inhibitor 4, is an efficient inhibitor of multidrug resistance (MDR) that exhibits inhibitory activity toward P-glycoprotein-mediated drug efflux. Multi-target kinase inhibitor 4 can be loaded into PEG-coated LNPs[1].
  • HY-10115R
    PI-103 (Standard) Inhibitor
    PI-103 (Standard) is the analytical standard of PI-103. This product is intended for research and analytical applications. 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[1][2][3][4].
  • HY-10115AR
    PI-103 Hydrochloride (Standard) Inhibitor
    PI-103 (Hydrochloride) (Standard) is the analytical standard of PI-103 (Hydrochloride). This product is intended for research and analytical applications. 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[1][2][3][4].
  • HY-10108R
    LY294002 (Standard) Inhibitor
    LY294002 (Standard) is the analytical standard of LY294002. This product is intended for research and analytical applications. 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[1]. LY294002 also inhibits CK2 with an IC50 of 98 nM[2]. 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[3].
  • 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[1].
  • HY-142944
    DNA-PK-IN-2 Inhibitor
    DNA-PK-IN-2 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-2 has the potential for the research of cancer diseases (extracted from patent WO2021136462A1, compound 1)[1].
  • HY-110109
    ETP-45658 Inhibitor 98.97%
    ETP-45658 is a potent PI3K inhibitor, with IC50s of 22.0 nM, 39.8 nM, 129.0 nM and 717.3 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. ETP-45658 also can inhibit DNA-PK (IC50=70.6 nM) and mTOR (IC50=152.0 nM). ETP-45658 can be used for the research of cancer[1][2].
  • HY-146565
    DNA-PK-IN-8 Inhibitor 99.74%
    DNA-PK-IN-8 is a highly potent, selective and orally active DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 value of 0.8 nM. DNA-PK-IN-8 exhibits synergistic antiproliferative activity against a series of cancer cell lines and significantly suppresses HL-60 tumor growth, when using in combination with Doxorubicin[1].
  • HY-122727
    STL127705 Inhibitor
    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[1][2].
  • HY-101667
    LTURM34 Inhibitor 99.35%
    LTURM34 is a specific DNA-PK inhibitor (IC50=34 nM). LTURM34 exhibits 170-fold selectivity for DNA-PK over PI3K. LTURM34 shows potent antiproliferative activity in a wide range of tumor cell lines[1].
  • HY-16124
    Canfosfamide Inhibitor
    Canfosfamide (TLK-286, TER286) is a glutathione analogue prodrug that is activated by glutathione S-transferase P1-1 and induces apoptosis. Canfosfamide also inhibits the catalytic kinase activity of DNA-dependent protein kinase (DNA-PK). Canfosfamide produces an anticancer alkylating agent and a glutathione derivative after activation. Canfosfamide can be used to research malignancies[1][2][3].
  • 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[1].
  • HY-13281
    PIK-75 hydrochloride Inhibitor
    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)[1][2]. PIK-75 hydrochloride induces apoptosis[3].
  • HY-144038
    DNA-PK-IN-5 Inhibitor
    DNA-PK-IN-5 is a potent inhibitor of DNA-PK. DNA-PK-IN-5 inhibits DNA-PKcs activity, thus greatly reducing tumor DNA repair and inducing cells to enter the apoptotic program. DNA-PK-IN-5 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 WO2021204111A1, compound 2)[1].
  • 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[1].