ku-0063794

Description: KU-0063794 is a novel, potent, cell permeable and selective inhibitor of mTOR (mammalian target of rapamycin) with potential anticancer activity. It inhibits both mTORC1 and mTORC2 with an IC50 of ca.10 nM. It does not suppress the activity of 76 other protein kinases or seven lipid kinases, including Class 1 PI3Ks (phosphoinositide 3-kinases) at 1000-fold higher concentrations. Ku-0063794 also inhibited phosphorylation of the T-loop Thr308 residue of Akt phosphorylated by PDK1. Ku-0063794 also suppressed cell growth and induced a G1-cell-cycle arrest. Ku-0063794 will be useful in delineating the physiological roles of mTOR and may have utility in treatment of cancers in which this pathway is inappropriately activated.

References: Biochem J. 2009 Jun 12; 421(1):29-42