DNA-activated protein kinase (DNA-PK; EC plays an important role in responding to agents and extracellular stress that threaten the DNA replication process[1]. It is a nuclear protein serine/threonine kinase that must bind to DNA double-strand breaks (DSB) to be active. The nonhomologous end-joining (NHEJ) pathway is considered the main pathway for DSB repair in mammalian cells, and is initiated by binding of DNA-dependent protein kinase (DNA-PK) regulatory subunits to free DNA ends, followed by recruitment of the DNA-dependent kinase catalytic subunit protein (DNA-PKcs) to DSBs. This assembly results in DNA-PK kinase activation. The DNA-PK complex serves as a platform that holds both DNA ends together and orchestrates DNA processing and ligation[2].DNA-PK inhibiting Axon Ligands™ are also listed in the section of theDNA-damage response.

[1] ATM,ATR andDNA-PK: initiators of the cellular genotoxic stress responses. J Yang, Y Yu, H Hamrick, PJ Duerksen-Hughes. Carcinogenesis 2003, 24, 1571-1580.
[2] Essential role forDNA-PK-mediated phosphorylation of NR4A nuclear orphan receptors inDNA double-strand break repair. M. Malewicz et al. Genes & Dev. 2011, 25, 2031-2040.

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Axon ID Name Description From price
4068 AZD7648 DNA-PK inhibitor €90.00
2604 KU-0060648 DNA-PK inhibitor €135.00
1584 KU-0060648 trihydrochloride DNA-PK inhibitor Inquire
3577 M-3814 DNA-PK inhibitor Inquire
1463 NU 7441 DNA-PK inhibitor €40.00

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