Chemical Name: 4-Ethyl-N-[4-[2-(4-morpholinyl)-4-oxo-4H-1-benzopyran-8-yl]-1-dibenzothienyl]-1-piperazineacetamide
Biological ActivityDual PI 3-K and DNA-PK inhibitor (IC50 values are <0.1, 0.5, 4 and 19 nM for PI 3-Kδ, PI 3-Kβ, PI 3-Kα and DNA-PK respectively). Inhibits proliferation of MCF7 cells in vitro and delays growth of MCF7 xenografts in mice. Also enhances CRISPR-Cas9-mediated homology-directed repair (HDR) efficiency ~2 to 4-fold, and decreases nonhomologous end-joining (NHEJ) frequency ~40%; maximum effect seen at 250 nM.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Chemosensitization of cancer cells by KU-0060648, a dual inhibitor of DNA-PK and PI-3K.
Munck et al.
Mol.Cancer Ther., 2012;11:1789
Radiosensitising agents for the radiotherapy of cancer: novel molecularly targeted approaches.
Dumont et al.
Expert Opin.Ther.Patents, 2009;19:775
Pharmacological inhibition of DNA-PK stimulates Cas9-mediated genome editing.
Robert et al.
Genome Med., 2015;7:93
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