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Submit ReviewKU 0060648
Description: Dual DNA-PK and PI 3-K inhibitor
Chemical Name: 4-Ethyl-N-[4-[2-(4-morpholinyl)-4-oxo-4H-1-benzopyran-8-yl]-1-dibenzothienyl]-1-piperazineacetamide
Purity: ≥97% (HPLC)
Biological Activity for KU 0060648
KU 0060648 is a dual 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.
Licensing Information
Sold under license from Cancer Research Technology Ltd.
Technical Data for KU 0060648
| M. Wt | 582.71 |
| Formula | C33H34N4O4S |
| Storage | Store at -20°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 881375-00-4 |
| PubChem ID | 11964036 |
| InChI Key | AATCBLYHOUOCTO-UHFFFAOYSA-N |
| Smiles | O=C1C3=C(C(C4=CC=C(NC(CN7CCN(CC)CC7)=O)C5=C4SC6=C5C=CC=C6)=CC=C3)OC(N2CCOCC2)=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Product Datasheets for KU 0060648
References for KU 0060648
References are publications that support the biological activity of the product.
Munck et al (2012) Chemosensitization of cancer cells by KU-0060648, a dual inhibitor of DNA-PK and PI-3K. Mol.Cancer Ther. 11 1789 PMID: 22576130
Dumont et al (2009) Radiosensitising agents for the radiotherapy of cancer: novel molecularly targeted approaches. Expert Opin.Ther.Patents 19 775 PMID: 19456277
Robert et al (2015) Pharmacological inhibition of DNA-PK stimulates Cas9-mediated genome editing. Genome Med. 7 93 PMID: 26307031
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Keywords: KU 0060648, KU 0060648 supplier, KU0060648, antitumor, antitumour, PI, 3-K, phosphoinositide, 3-kinases, inhibits, inhibitors, DNA-PK, DNA-dependent, protein, CRISPR, Cas9, HDR, NHEJ, homology, directed, repair, nonhomologous, end, joining, hematopoietic, haematopoietic, stem, cells, HSC, Protein, Kinase, 3-Kinase, Checkpoint, Control, Kinases, Reagents, Hematopoietic, Stem, Cells, 4840, Tocris Bioscience
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Cell Cycle and DNA Damage Research Product Guide
This product guide provides a review of the cell cycle and DNA damage research area and lists over 150 products, including research tools for:
- Cell Cycle and Mitosis
- DNA Damage Repair
- Targeted Protein Degradation
- Ubiquitin Proteasome Pathway
- Chemotherapy Targets
Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.