mTOR Inhibitor, Ku-0063794

• CAT Number: I005576
• CAS Number: 938440-64-3
• Molecular Formula: C₂₅H₃₁N₅O₄
• Molecular Weight: 465.54
• Purity: ≥95%
• Target: mTOR
• Solubility: DMSO ≥10mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL
• Storage: 3 years -20C powder
• IC50: ~10 nM
• InChI: InChI=1S/C25H31N5O4/c1-16-13-30(14-17(2)34-16)25-27-23-20(24(28-25)29-8-10-33-11-9-29)5-6-21(26-23)18-4-7-22(32-3)19(12-18)15-31/h4-7,12,16-17,31H,8-11,13-15H2,1-3H3/t16-,17+
• InChIKey: RFSMUFRPPYDYRD-CALCHBBNSA-N
• SMILES: CC1CN(CC(O1)C)C2=NC3=C(C=CC(=N3)C4=CC(=C(C=C4)OC)CO)C(=N2)N5CCOCC5

KU-0063794 is a selective inhibitor of mammalian target of rapamycin (mTOR) (IC50 ~10 nM for mTORC1 and mTORC2 respectively); no effect on PI3Ks. 


KU-0063794 displays no activity at PI 3-kinase or 76 other kinases tested. Inhibits activation and hydrophobic motif phosphorylation of Akt, S6K and SGK, but not RSK. KU-0063794 suppresses cell growth and induces G1 cell cycle arrest in vitro.

Reference

1:Autophagy inhibition sensitizes KU-0063794-mediated anti-HepG2 hepatocellular carcinoma cell activity in vitro and in vivo. Yongxi T, Haijun H, Jiaping Z, Guoliang S, Hongying P.Biochem Biophys Res Commun. 2015 Sep 25;465(3):494-500. doi: 10.1016/j.bbrc.2015.08.045. Epub 2015 Aug 14. PMID: 26278819 2:Potent dual inhibitors of TORC1 and TORC2 complexes (KU-0063794 and KU-0068650) demonstrate in vitro and ex vivo anti-keloid scar activity. Syed F, Sanganee HJ, Singh S, Bahl A, Bayat A.J Invest Dermatol. 2013 May;133(5):1340-50. doi: 10.1038/jid.2012.483. Epub 2013 Jan 10. Erratum in: J Invest Dermatol. 2014 Sep;134(9):2475. Singh, Subir [Added]. PMID: 23303455 Free PMC Article3:Ku-0063794 is a specific inhibitor of the mammalian target of rapamycin (mTOR). García-Martínez JM, Moran J, Clarke RG, Gray A, Cosulich SC, Chresta CM, Alessi DR.Biochem J. 2009 Jun 12;421(1):29-42. doi: 10.1042/BJ20090489. PMID: 19402821 Free PMC Article