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Description: KU0060648 is a novel, potent and selective inhibitor of DNA-dependent protein kinase (DNA-PK) with IC50 of 8.6 nM and with 20-1000 fold selectivity for DNA-PK over other PIKKs and a panel of 60 kinases. KU-0060648 enhances HDR efficiency and attenuates NHEJ frequency. KU-0060648 is also considered as a dual inhibitor of DNA-PK and PI-3K. KU-0060648 inhibited cellular DNA-PK autophosphorylation with IC(50) values of 0.019 umol/L (MCF7 cells) and 0.17 umol/L (SW620 cells), and PI-3K-mediated AKT phosphorylation with IC(50) values of 0.039 umol/L (MCF7 cells) and more than 10 umol/L (SW620 cells). KU-0060648 inhibits hepatocellular carcinoma cells through DNA-PKcs-dependent and DNA-PKcs-independent mechanisms.
References: Oncotarget. 2016 Mar 29; 7(13):17047-59.
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