Cat. #152709
Dual DNA-PK/PI3K inhibitor KU-0060648 Small Molecule (Tool Compound)
Cat. #: 152709
Sub-type: Inhibitor
Availability: Please enquire for quantities and pricing
Application: KU-0060648 enhances the anti-tumour activity of etoposide in both MCF7 and SW620 xenograft models, and has single-agent activity in the MCF7 xenograft model. KU-0060648 exhibits differential effects on growth inhibition, but is not profoundly cytotoxic in a panel of human cancer cell lines. It inhibits DNA-PK and PI-3K with greater potency in MCF7 than SW620 cell using cell-based assays. Five-day exposure to 1 mM KU-0060648 inhibits cell proliferation by more than 95% in MCF7 cells but only b...
This fee is applicable only for non-profit organisations. If you are a for-profit organisation or a researcher working on commercially-sponsored academic research, you will need to contact our licensing team for a commercial use license.
Contributor
Inventor: Laurent Rigoreau
Institute: Newcastle University
Tool Details
*FOR RESEARCH USE ONLY (for other uses, please contact the licensing team)
- Tool name: Dual DNA-PK/PI3K inhibitor KU-0060648 Small Molecule (Tool Compound)
- Research fields: Cancer;Cell biology
- Molecular formula: C33H34N4O4S
- Tool sub type: Inhibitor
- Primary target: Dual PI 3-K and DNA-PK inhibitor
- Description: KU-0060648 is a dual PI3-K and DNA-PK inhibitor (IC50 values are <0.1, 0.5, 4 and 19 nM for PI 3-Kd, PI 3-K?, PI 3-Ka and DNA-PK respectively). It inhibits proliferation of MCF7 cells in vitro and delays growth of MCF7 xenografts in mice. KU-0060648 can also enhance CRISP-Cas9-mediated homology-directed repair (HDR) efficiency, and attenuate nonhomologous end-joining (NHEJ).
- Application: KU-0060648 enhances the anti-tumour activity of etoposide in both MCF7 and SW620 xenograft models, and has single-agent activity in the MCF7 xenograft model. KU-0060648 exhibits differential effects on growth inhibition, but is not profoundly cytotoxic in a panel of human cancer cell lines. It inhibits DNA-PK and PI-3K with greater potency in MCF7 than SW620 cell using cell-based assays. Five-day exposure to 1 mM KU-0060648 inhibits cell proliferation by more than 95% in MCF7 cells but only b...
- Purpose: Inhibitor
- Molecular weight: 582.71
- Solubility: Soluble to 100 mM in 2eq.HCl
Handling
- Purity: 582.71 g/mol
- Storage conditions: Store at -20° C
- Shipping conditions: Dry Ice
Target Details
- Primary target: Dual PI 3-K and DNA-PK inhibitor
- Ic50: inhibitor of DNA-PK and PI3Kι, PI3Kβ, PI3Kδ with IC50 of 8.6 nM and 4 nM, 0.5 nM, 0.1 nM respectively, less inhibition of PI3Kγ with IC50 of 0.59 ΟM.
Application Details
- Application: KU-0060648 enhances the anti-tumour activity of etoposide in both MCF7 and SW620 xenograft models, and has single-agent activity in the MCF7 xenograft model. KU-0060648 exhibits differential effects on growth inhibition, but is not profoundly cytotoxic in a panel of human cancer cell lines. It inhibits DNA-PK and PI-3K with greater potency in MCF7 than SW620 cell using cell-based assays. Five-day exposure to 1 mM KU-0060648 inhibits cell proliferation by more than 95% in MCF7 cells but only b...
References
- Robert et al. 2015. Genome Med. 7(1):93. PMID: 26307031.
- Pharmacological inhibition of DNA-PK stimulates Cas9-mediated genome editing.
- Munck et al. 2012. Mol Cancer Ther. 11(8):1789-98. PMID: 22576130.
- Chemosensitization of cancer cells by KU-0060648, a dual inhibitor of DNA-PK and PI-3K.
