Dual DNA-PK/PI3K inhibitor KU-0060648 Small Molecule (Tool Compound)

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

Contributors

Inventor Institute
Laurent Rigoreau Newcastle University
Cat. #: 152709
Tool sub type: Inhibitor
Research Fields: Cancer;Cell biology
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
Product 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).
Molecular weight: 582.71
Primary target: Dual PI 3-K and DNA-PK inhibitor
Storage conditions: Store at -20° C
Shipping conditions: Dry Ice
Solubility: Soluble to 100 mM in 2eq.HCl
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.

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Structure of KU-0060648

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