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-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.
    LTURM34
  • HY-107834
    PIK-75
    		Inhibitor 99.94%
    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-19977
    YU238259
    		Inhibitor 98.86%
    YU238259 is an inhibitor of homology-dependent DNA repair (HDR), used for cancer research.
    YU238259
  • 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.
    ETP-45658
  • HY-162472
    XRD-0394
    		Inhibitor 98.54%
    XRD-0394 is a potent and orally active dual ATM and DNA-PKcs inhibitor with IC50s of 0.39 nM and 0.89 nM, respectively. XRD-0394 shows selectivity over other PIKK and PI3K family members. XRD-0394 significantly enhances tumor cell killing in vitro and in vivo under therapeutic ionizing radiation conditions. XRD-0394 can potentiate the effects of PARP and topoisomerase I inhibitors in vitro.
    XRD-0394
  • HY-19341
    Compound 401
    		Inhibitor 99.97%
    Compound 401 is a synthetic inhibitor of DNA-PK (IC50 = 0.28 μM) that also targets mTOR but not PI3K in vitro.
    Compound 401
  • HY-100706
    AMA-37
    		Inhibitor 99.48%
    AMA-37, an Arylmorpholine analog, is ATP-competitive DNA-PK inhibitor, with IC50 values of 0.27 μM (DNA-PK), 32 μM (p110α), 3.7 μM (p110β), and 22 μM (p110γ), respectively.
    AMA-37
  • HY-19939S2
    (R)-VX-984
    		99.88%
    (R)-VX-984 is the (R)-enantiomer of VX-984. VX-984 is a potent DNA-PK inhibitor.
    (R)-VX-984
  • HY-100707
    IC 86621
    		Inhibitor 99.06%
    IC 86621 is a potent DNA-dependent protein kinase (DNA-PK) inhibitor, with an IC50 of 120 nM. IC 86621 also acts as a selective and reversible ATP-competitive inhibitor.IC 86621 inhibits DNA-PK mediated cellular DNA double-strand break (DSB) repair (EC50=68 µM). IC 86621 increases DSB-induced antitumor activity without cytotoxic effects. IC 86621 can protects rheumatoid arthritis (RA) T cells from apoptosis.
    IC 86621
  • HY-163134
    DNA-PK-IN-12
    		Inhibitor 99.63%
    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-158122
    Lys(CO-C3-p-I-Ph)-O-tBu
    		98.14%
    Lys(CO-C3-p-I-Ph)-O-tBu is a pharmacokinetic modifier (PK modifier) that can improve the PK properties of PSMA ligand molecules. Lys(CO-C3-p-I-Ph)-O-tBu can increase the residence time of PSMA ligand in plasma by increasing its binding capacity to albumin. Lys(CO-C3-p-I-Ph)-O-tBu also reduces salivary gland absorption, possibly extending the half-life of the active compound. Ac-PSMA-trillium is a suitable PSMA-targeting compound that has different biological applications after modification with different radioactive isotopes. If labeled with 111In, it can be used as DOTA chelating agent and imaging agent. Or labeled with 225Ac as a Macropa chelator for targeted radionuclide therapy (TRT) in the study of metastatic castration-resistant prostate cancer (mCRPC).
    Lys(CO-C3-p-I-Ph)-O-tBu
  • HY-158118
    Lys(CO-C3-p-I-Ph)-OMe
    Lys(CO-C3-p-I-Ph)-OMe is a pharmacokinetic modifier (PK modifier) that can improve the PK properties of PSMA ligand molecules (such as Ac-PSMA-trillium). Lys(CO-C3-p-I-Ph)-OMe can increase the residence time of Ac-PSMA-trillium in plasma by increasing its binding capacity to albumin. Lys(CO-C3-p-I-Ph)-OMe also reduces salivary gland absorption of Ac-PSMA-trillium, potentially extending its half-life. Ac-PSMA-trillium is a suitable PSMA-targeting compound that has different biological applications after modification with different radioactive isotopes. If labeled with 111In, it can be used as DOTA chelating agent and imaging agent. Or labeled with 225Ac as a Macropa chelator for targeted radionuclide therapy (TRT) in the study of metastatic castration-resistant prostate cancer (mCRPC).
    Lys(CO-C3-p-I-Ph)-OMe
  • 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.
    DNA-PK-IN-8
  • HY-145427
    NU5455
    		Inhibitor
    NU5455 is a potent, selective, and orally active inhibitor of DNA-PKcs. NU5455 administration increases both the efficacy and the toxicity of a parenterally administered topoisomerase inhibitor. NU5455 enhances the activity of Doxorubicin released locally in liver tumor xenografts without inducing any adverse effect.
    NU5455
  • HY-142471A
    ZL-2201
    		Inhibitor 99.16%
    ZL-2201 is a potent DNA-PK inhibitor with an IC50 of 1 nM (WO2021104277A1, compound 5).
    ZL-2201
  • 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).
    DNA-PK-IN-2
  • 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.
    Canfosfamide
  • 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).
    DNA-PK-IN-5
  • 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-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
Cat. No. Product Name / Synonyms Application Reactivity