Application
KU 0063794 has been used:
- as a mammalian target of rapamycin (mTOR) inhibitor to study the effects of follicular stimulating hormone (FSH) in mTOR phosphorylation and vascular cell adhesion molecule-1 (VCAM-1) expression in human umbilical vascular endothelial cells (HUVECs)
- as a mTOR inhibitor to treat effector memory (EM) CD8+ T cells for metabolic flux analysis
- as an autophagy inducer to demonstrate the utility of p62 and LC3B-II quantification in HEK293T cells and primary cultures of rat neurons and astrocytes using time-resolved fluorescence resonance energy transfer (TR-FRET)
Biochem/physiol Actions
KU 0063794 induces autophagy. It is cell-permeant and suppresses activation and hydrophobic motif phosphorylation of protein kinase B (Akt), p70 ribosomal S6 kinase (S6K) and serum and glucocorticoid protein kinase (SGK).
KU 0063794 is a potent and selective inhibitor of mammalian target of rapamycin (mTOR) (IC50 ~10 nM for both mTORC1 and mTORC2) that inhibits both mTORC1 and mTORC2 in vitro and in vivo (IC50 ~10 nM for both mTORC1 and mTORC2). KU 0063794 does not significantly inhibit 76 other protein kinases tested as well as seven lipid kinases including PI3K and AKT.
KU 0063794 is a potent and selective inhibitor of mammalian target of rapamycin (mTOR); inhibits both mTORC1 and mTORC2 in vitro and in vivo.
Features and Benefits
This compound is featured on the PKB/Akt page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
| Quality Level | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: >2 mg/mL (warmed) |
| storage temp. | 2-8°C |
| SMILES string | COc1ccc(cc1CO)-c2ccc3c(nc(nc3n2)N4C[C@H](C)O[C@H](C)C4)N5CCOCC5 |
| 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+ |
| InChI key | RFSMUFRPPYDYRD-CALCHBBNSA-N |

