DNA-PK (DNA-dependent protein kinase) is a nuclear serine/threonine protein kinase made up of a heterodimeric DNA-targeting subunit Ku and a large catalytic subunit (DNA-PKcs). The Nonhomologous End-Joining (NHEJ) pathway of DNA double-strand break repair contains a significant amount of DNA-PK. DNA-PK plays significant roles in the regulation of various DNA transactions, including transcription, replication, and DNA repair, as well as in the maintenance of telomeres. DNA-PK specifically requires association with DNA for its kinase activity.
Artemis, DNA ligase IV, and other NHEJ factors that are involved in end-processing and ligation are attracted to DSB ends where DNA-PK is assembled. Ku proteins act as early sensors and confer high affinities to DSB ends within the DNA-PK complex. The activation of DNA-PKcs, a member of the phosphatidylinositol 3-kinase-related kinase (PIKK) family, is caused by the subsequent recruitment of DNA-PKcs to DSBs via the Ku proteins. Several substrates, including H2AX, XRCC4, Artemis, and most importantly, DNA-PKcs itself, are phosphorylated by DNA-PKcs after it is activated. It has been demonstrated that NHEJ is mediated by DNA-PKcs autophosphorylation, which takes place at numerous Ser/Thr residues throughout the kinase.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V52954 | (R)-VX-984 ((R)-M9831) | 2448475-19-0 | (R)-VX-984 is the R-enantiomer of VX-984. |
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V4344 | AZD-7648 | 2230820-11-6 | AZD-7648 (AZD7648) is a novel, potent and selectiveDNA-PK (DNA-dependent protein kinase) inhibitor with potential anticancer/antitumor activity. |
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V52979 | BAY-8400 | 2763602-59-9 | BAY-8400 is an orally bioactive, potent and specific DNA-dependent protein kinase (DNA-PK) inhibitor (IC50=81 nM). |
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V4345 | CC-115 HYDROCHLORIDE | 1300118-55-1 | CC-115 hydrochloride (CC115 HCl) isa novel and potent dual inhibitor of DNA-PK (DNA-dependent protein kinase) and mTOR (mammalian target of rapamycin) withIC50s of 13 nM and 21 nM, respectively and with potential antineoplastic activity. |
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V3996 | COMPOUND 401 | 168425-64-7 | Compound 401 is a potent synthetic inhibitor of DNA-dependent protein kinase (DNA-PK,IC50= 0.28 μM) that also targets mTOR but not PI3K in vitro. |
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V52169 | DNA-PK-IN-10 | 2919315-89-0 | DNA-PK-IN-10 is a DNA-PK inhibitor. |
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V52168 | DNA-PK-IN-8 | 2823369-81-7 | DNA-PK-IN-8 (compound DK1) is a specific and orally bioactive DNA-dependent protein kinase (DNA-PK) inhibitor (antagonist) with IC50 of 0.8 nM. |
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V4346 | KU-0060648 | 881375-00-4 | KU0060648 (KU-0060648) is a novel, potent and selective inhibitor of DNA-dependent protein kinase (DNA-PK) with anticancer activity. |
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V0254 | KU-0060648 HCL | KU0060648 HCl is a novel, potent and dual inhibitor of DNA-dependent protein kinase (DNA-PK) and PI3Kα/β/δ (Phosphoinositide 3-kinases) with potential antitumor activity. | |
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V24465 | LTURM-34 | 1879887-96-3 | LTURM34 is a specific DNA-PK inhibitor (IC50=34 nM). |
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V0253 | NU7026 | 154447-35-5 | NU7026 is a novel and potent DNA-PK (DNA-dependent protein kinase) with potential antitumor activity. |
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V3225 | PIK-75 | 372196-67-3 | PIK-75 is a p110α inhibitor with IC50 of 5.8 nM, which is 200-fold more potent than p110β. |
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V0200 | PP121 | 1092788-83-4 | PP-121 is a novel, potent and selective multi-targeted RTK (receptor tyrosine kinases) inhibitor with potential antitumor activity. |
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V14351 | YU238259 | 1943733-16-1 | YU238259 (YU-238259) Is a novel and potent HDR (Homology-Dependent DNA Repair) inhibitor with anticancer activity. |
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V55765 | ZL-2201 | 2865115-39-3 | ZL-2201 is a potent DNA-PK inhibitor (antagonist) with IC50 of 1 nM (WO2021104277A1, compound 5). |
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