DNA-PK
DNA-dependent protein kinase
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.
All Product Categories
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DNA-PK Related Products (75)
Related Products (75)
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Antibodies (5)
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DNA-PK-IN-15
0 ImagesCat. No.: HY-169248CAS No.: 2663852-17-1DNA-PK-IN-15 (compound 6) is an inhibitor of DNA-PK with an IC50 value of 0.08 nM.
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DNA-PK-IN-2
0 ImagesCat. No.: HY-142944CAS No.: 2665720-22-7DNA-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).
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Canfosfamide
0 ImagesCat. No.: HY-16124CAS No.: 158382-37-7Synonyms: TLK-286; TER286Canfosfamide (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.
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Nedisertib (GMP)
0 ImagesCat. No.: HY-101570GCAS No.: 1637542-33-6Synonyms: Peposertib (GMP); M3814 (GMP)Nedisertib (GMP) (Peposertib (GMP)) is Nedisertib (HY-101570) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Nedisertib is an orally active selective DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 value of less than 3 nM. Nedisertib also acts as a modulator of ABCG2, capable of reversing ABCG2-mediated multidrug resistance (MDR), thus providing new strategies for combination therapy. By inhibiting DNA double-strand break repair, Nedisertib can enhance the efficacy of chemotherapy and radiotherapy. Nedisertib exhibits antitumor activity.
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DNA-PK-IN-5
0 ImagesCat. No.: HY-144038CAS No.: 2719736-43-1DNA-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).
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SU-11752
0 ImagesCat. No.: HY-114923CAS No.: 688036-19-3SU-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.
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AZD-7648 (GMP)
0 ImagesCat. No.: HY-111783GCAS No.: 2230820-11-6AZD-7648 (GMP) is AZD-7648 (HY-111783) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. 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.
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NU-7031
0 ImagesCat. No.: HY-123118CAS No.: 79105-88-7
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Multi-target kinase inhibitor 4
0 ImagesCat. No.: HY-172771Multi-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.
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DNA-PK-IN-3
0 ImagesCat. No.: HY-144036CAS No.: 2734846-19-4DNA-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).
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PP487
0 ImagesCat. No.: HY-15268CAS No.: 1092787-12-6
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DNA-PK-IN-1
0 ImagesCat. No.: HY-142943CAS No.: 2663850-40-4DNA-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).
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DNA-PK-IN-9
0 ImagesCat. No.: HY-146566CAS No.: 3034675-75-4DNA-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.
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ZL-2201 free base
0 ImagesCat. No.: HY-142471CAS No.: 2646592-18-7ZL-2201 free base is a potent DNA-PK inhibitor with an IC50 of 1 nM (WO2021104277A1, compound 5).
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DNA-PK-IN-14
0 ImagesCat. No.: HY-162692CAS No.: 2766001-96-9DNA-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.
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DNA-PK-IN-4
0 ImagesCat. No.: HY-144037CAS No.: 2722645-10-3DNA-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).
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Panulisib
0 ImagesCat. No.: HY-16769CAS No.: 1356033-60-7Synonyms: P7170; AK151761Panulisib (P7170; AK151761) is an orally active inhibitor of PI3K (IC50 = 2.2 nM) and mTOR (IC50 = 4.4 nM). Panulisib inhibits ALK1 and DNA-PK, two enzymes that respectively participate in angiogenesis and DNA repair, with IC50 values of 47 nM and 1.5 nM respectively. Panulisib inhibits cell proliferation and apoptosis. Panulisib can be used for research on breast cancer and non-small cell lung cancer.
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p53 Stabilizer 2
0 ImagesCat. No.: HY-172915CAS No.: 2531685-87-5
