KU-0063794

KU-0063794 is a potent and selective mTOT inhibitor, which inhibits both mTORC1 and mTORC2 with an IC50 of approximately 10 nM, but 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 is cell permeant, suppresses activation and hydrophobic motif phosphorylation of Akt, S6K and SGK, but not RSK (ribosomal S6 kinase), an AGC kinase not regulated by mTOR. Ku-0063794 also inhibited phosphorylation of the T-loop Thr308 residue of Akt phosphorylated by PDK1 (3-phosphoinositide-dependent protein kinase-1). 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.

Related Products:  

Everolimus; Temsirolimus; PI-103; Torin 1; PF-04691502; Apitolisib; Torin 2; BGT226; Palomid 529; Deforolimus; Rapamycin; Tacrolimus

[1]. Garcia-Martinez et al. Ku-0063794 is a specific inhibitor of the mammalian target of rapamycin (mTOR). Biochem.J. (2009)421 29.

[2]. Collak FK, et al. Threonine-120 phosphorylation regulated by phosphoinositide-3-kinase/Akt and mammalian target of rapamycin pathway signaling limits the antitumor activity of mammalian sterile 20-like kinase 1.J Biol Chem. 2012 Jul 6;287(28):23698-709. E

[3]. Haagensen EJ, et al. The synergistic interaction of MEK and PI3K inhibitors is modulated by mTOR inhibition. Br J Cancer. 2012 Apr 10;106(8):1386-94.