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
-
DNA-PK Related Products (78)
Related Products (78)
-
Antibodies (5)
-
IC-87361
0 ImagesCat. No.: HY-122226CAS No.: 404011-02-5IC-87361 is a DNA-dependent protein kinase (DNA-PKcs) inhibitor with an IC50 of 35 nM, and radiosensitizer. IC-87361 inhibits the catalytic activity of DNA-PKcs and blocks non-homologous end joining (NHEJ) DNA double-strand break repair. IC-87361 can be used for the research of lung cancer and melanoma.
-
DNA-PK-IN-16
0 ImagesCat. No.: HY-181848DNA-PK-IN-16 is an orally active DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 of 10.2 nM. DNA-PK-IN-16 induces the upregulation of γH2A.X, a biomarker of DNA double-strand breaks. DNA-PK-IN-16 exhibits antiproliferative activity in various cancer cell lines. DNA-PK-IN-16 enhances the infiltration of CD8+ T cells in tumor tissues through synergistic action with anti-PD-L1 monoclonal antibody. DNA-PK-IN-16 is applicable for cancer research.
-
DNA-PK-IN-6
0 ImagesCat. No.: HY-144039CAS No.: 2711810-41-0DNA-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/HDAC6-IN-1
0 ImagesCat. No.: HY-181678DNA-PK/HDAC6-IN-1 is a selcetive and orally active dual DNA-PK and HDAC6 inhibitor with IC50 values of 84.2 and 64.8 nM. DNA-PK/HDAC6-IN-1 suppresses cancer cells proliferation, induces cancer cell cycle G2/M arrest, apoptosis, and decreases the mitochondrial membrane potential. DNA-PK/HDAC6-IN-1 induces DNA damage and elevates γ-H2AX levels. DNA-PK/HDAC6-IN-1 exhibits antitumor efficacy in AML animal mouse model. DNA-PK/HDAC6-IN-1 can be used for the research of acute myeloid leukemia.
-
PIK-75 (Standard)
0 ImagesCat. No.: HY-107834RCAS No.: 372196-67-3PIK-75 (Standard) is the analytical standard of PIK-75 (HY-107834). This product is intended for research and analytical applications. 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.
-
SF2523 (Standard)
0 ImagesCat. No.: HY-101146RCAS No.: 1174428-47-7SF2523 (Standard) is the analytical standard of SF2523 (HY-101146). This product is intended for research and analytical applications. SF2523 is a highly selective and potent inhibitor of PI3K with IC50s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.
-
Nedisertib (Standard)
0 ImagesCat. No.: HY-101570RCAS No.: 1637542-33-6Synonyms: Peposertib (Standard); M3814 (Standard)Nedisertib (Standard) is the analytical standard of Nedisertib (HY-101570). This product is intended for research and analytical applications. Nedisertib (Peposertib) 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.
-
LTURM34 (Standard)
0 ImagesCat. No.: HY-101667RCAS No.: 1879887-96-3LTURM34 (Standard) is the analytical standard of LTURM34 (HY-101667). This product is intended for research and analytical applications. 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.
-
ETP-45658 (Standard)
0 ImagesCat. No.: HY-110109RCAS No.: 1198357-79-7ETP-45658 (Standard) is the analytical standard of ETP-45658 (HY-110109). This product is intended for research and analytical applications. 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.
-
PI-103 (Standard)
0 ImagesPI-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.
-
AZD-7648 (Standard)
0 ImagesCat. No.: HY-111783RCAS No.: 2230820-11-6
-
LY294002 hydrochloride (Standard)
0 ImagesLY294002 (hydrochloride) (Standard) is the analytical standard of LY294002 (hydrochloride). This product is intended for research and analytical applications. LY294002 hydrochloride is a potent and broad-spectrum PI3K inhibitor, with IC50 values of 0.5, 0.57, and 0.97 μM for P110α, P110δ and P110β, respectively. LY294002 hydrochloride also inhibits CK2 with an IC50 of 98 nM. LY294002 hydrochloride can be used for pancreatic cancer research.
-
Sulfabenzamide (Standard)
0 ImagesSulfabenzamide (N-Sulfanilylbenzamide) (Standard) is the analytical standard of Sulfabenzamide (HY-B0960). This product is intended for research and analytical applications. Sulfabenzamide is a sulfonamide antibacterial agent. Sulfabenzamide exhibit antibacterial activity against Staphylococcus aureus (ATCC 25923) and Escherichia coli (ATCC 8739). Sulfabenzamide can promote autophagic cell autophagy in breast cancer cells through p53/ DRAM pathway. Sulfabenzamide increases caspase-3 activity, deactivates PARP1 and DNA-PK, downregulates AKT1 and AKT2. Sulfabenzamide can be used for the researches of breast cancer and bacterial infections.
-
AMA-37 (Standard)
0 ImagesCat. No.: HY-100706RCAS No.: 404009-46-7AMA-37 (Standard) is the analytical standard of AMA-37 (HY-100706). This product is intended for research and analytical applications. 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.
-
OK-1035
0 ImagesCat. No.: HY-108975CAS No.: 98293-88-0OK-1035 is a selective DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 of 100 μM.
-
NU-7163
0 ImagesCat. No.: HY-116621CAS No.: 503468-03-9NU-7163 is an ATP-competitive DNA-PK inhibitor (IC50=0.19 μM; Ki=24 nM). NU-7163 enhances the cytotoxicity of ionizing radiation against the HeLa human tumor cell line in vitro.
-
KU-57788 (Standard)
0 ImagesCat. No.: HY-11006RCAS No.: 503468-95-9Synonyms: NU7441 (Standard)KU-57788 (Standard) is the analytical standard of KU-57788 (HY-11006). This product is intended for research and analytical applications. 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.
-
PI-103 Hydrochloride (Standard)
0 ImagesCat. No.: HY-10115ARCAS No.: 371935-79-4PI-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.
