Cat. No. 4840
Chemical Name: 4-Ethyl-N-[4-[2-(4-morpholinyl)-4-o
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.
Licensing InformationSold under license from Cancer Research Technology Ltd.
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.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
Robert et al (2015) Pharmacological inhibition of DNA-PK stimulates Cas9-mediated genome editing. Genome Med. 7 93. PMID: 26307031.
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.
If you know of a relevant reference for this product please let us know.
Citations are publications that use Tocris products.
Do you know of a great paper that uses KU 0060648 from Tocris? If so please let us know.
View Related Products by Target
View Related Products by Product Action
Keywords: 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, Tocris Bioscience, DNA-Dependent Protein Kinase Inhibitor products
Find multiple products by catalog number
New Products in this Area
Potent and selective allosteric activator of AMPKPerifosine
PKB/Akt inhibitor; also modulates Kv2.1 currentRAF 265
Raf kinase and VEGFR-2 inhibitorCZC 25146
Potent LRRK2 inhibitorRo 3280
Potent and selective PLK1 inhibitorRMM 46
MSK/RSK family kinase inhibitorLTURM 34
Potent DNA-PK inhibitorMLi-2
Potent and selective LRRK2 inhibitorLTURM 36
PI 3-kinase δ inhibitorPI 3065
Potent and selective PI 3-kinase p110δ inhibitorAZ PFKFB3 67
Potent and selective PFKFB3 inhibitorSTOCK2S 26016
Lysine deficient protein kinase (WNK) signaling inhibitorrac-CCT 250863
Potent Nek2 inhibitorRoscovitine
Potent, selective cyclin-dependent kinase inhibitorEnzastaurin
Potent PKCβ inhibitorBMS 265246
Potent cdk1/2 inhibitorAutocamtide-2-related inhibitory peptide, myristoylated
CaM kinase II inhibitor; enhanced cell permeable derivative of Autocamtide-2-related inhibitory peptide
Follow @Tocris on Twitter
Tocris is now actively tweeting. For regular updates on news, events and special offers, follow @Tocris on Twitter.