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.
Sold under license from Cancer Research Technology Ltd.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 582.71. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.72 mL||8.58 mL||17.16 mL|
|5 mM||0.34 mL||1.72 mL||3.43 mL|
|10 mM||0.17 mL||0.86 mL||1.72 mL|
|50 mM||0.03 mL||0.17 mL||0.34 mL|
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, Protein, Kinase, 3-Kinase, Checkpoint, Control, Kinases, Reagents, 4840, Tocris Bioscience
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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. Adapted from the 2015 Cancer Product Guide, Edition 3, 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.