KU 0063794
Chemical Name: rel-5-[2-[(2R,6S)-2,6-dimethyl-4-morpholinyl]-4-(4-morpholinyl)pyrido[2,3-d]pyrimidin-7-yl]-2-methoxybenzenemethanol
Purity: ≥97%
Biological Activity
KU 0063794 is a selective inhibitor of mammalian target of rapamycin (mTOR) (IC50 ~10 nM for mTORC1 and mTORC2). 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. Suppresses cell growth and induces G1 cell cycle arrest in vitro.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Nitric oxide regulates AKT phosphorylation and nuclear translocation in cultured retinal cells.
Mejia-Garcia T, Portugal C, Encarnacao T, Prado M, Paes-de-Carvalho R
Cell Signal, 2013;25(12):2424-39. -
Mechanistic target of rapamycin inhibition extends cellular lifespan in dendritic cells by preserving mitochondrial function.
Amiel E, Everts B, Fritz D, Beauchamp S, Ge B, Pearce E, Pearce E
J Immunol, 2014;193(6):2821-30. -
Targeted NF1 cancer therapeutics with multiple modes of action: small molecule hormone-like agents resembling the natural anticancer metabolite, 2-methoxyoestradiol.
Shen Y, Upadhyayula R, Cevallos S, Messick R, Hsia T, Leese M, Jewett D, Ferrer-Torres D, Roth T, Dohle W, Potter B, Barald K
Br J Cancer, 2015;113(8):1158-67. -
Insulin Receptor and GPCR Crosstalk Stimulates YAP via PI3K and PKD in Pancreatic Cancer Cells
F Hao, Q Xu, Y Zhao, JV Stevens, SH Young, J Sinnett-Sm, E Rozengurt
Mol. Cancer Res., 2017;0(0):. -
SynGAP regulates protein synthesis and homeostatic synaptic plasticity in developing cortical networks.
Wang C, Held R, Hall B
PLoS ONE, 2013;8(12):e83941. -
Ku-0063794 is a specific inhibitor of the mammalian target of rapamycin (mTOR).
Garcia-Martinez et al.
Biochem.J., 2009;421:29
Product Datasheets
Citations for KU 0063794
The citations listed below are publications that use Tocris products. Selected citations for KU 0063794 include:
14 Citations: Showing 1 - 10
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The innate immune kinase TBK1 directly increases mTORC2 activity and downstream signaling to Akt.
Authors: Ian E Et al.
J Biol Chem 2021;297:100942
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CDK8 Fine-Tunes IL-6 Transcriptional Activities by Limiting STAT3 Resident Time at the Gene Loci.
Authors: Ignacio Et al.
Cell Rep 2020;33:108545
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The 3-Phosphoinositide-Dependent Protein Kinase 1 Inhibits Rod Photoreceptor Development.
Authors: Xing Et al.
Front Cell Dev Biol 2018;6:134
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The IKK-related kinase TBK1 activates mTORC1 directly in response to growth factors and innate immune agonists.
Authors: Bodur Et al.
EMBO J 2018;37:19
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SYK kinase mediates brown fat differentiation and activation.
Authors: Lei Et al.
Nat Commun 2017;8:2115
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mTORC1 and CK2 coordinate ternary and eIF4F complex assembly.
Authors: Gandin Et al.
Nat Commun 2016;7:11127
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Insulin promotes proliferation and fibrosing responses in activated pancreatic stellate cells.
Authors: Ling Et al.
Am J Physiol Gastrointest Liver Physiol 2016;311:G675-G687
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The cytotoxic T cell proteome and its shaping by the kinase mTOR.
Authors: Hukelmann Et al.
J Biol Chem 2016;17:104
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mTOR activates the VPS34-UVRAG complex to regulate autolysosomal tubulation and cell survival.
Authors: Munson Et al.
Nat Immunol 2015;34:2272
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A novel MEK-ERK-AMPK signaling axis controls chemokine receptor CCR7-dependent survival in human mature dendritic cells.
Authors: López-Cotarelo Et al.
Proc Natl Acad Sci U S A 2015;290:827
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SynGAP regulates protein synthesis and homeostatic synaptic plasticity in developing cortical networks.
Authors: Wang Et al.
PLoS One 2014;8:e83941
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Targeting mTOR to overcome epidermal growth factor receptor tyrosine kinase inhibitor resistance in non-small cell lung cancer cells.
Authors: Fei Et al.
PLoS One 2013;8:e69104
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ATP-competitive mTOR kinase inhibitors delay plant growth by triggering early differentiation of meristematic cells but no developmental patterning change.
Authors: Montané and Menand
EMBO J 2013;64:4361
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Regulation of OSR1 and the sodium, potassium, two chloride cotransporter by convergent signals.
Authors: Sengupta Et al.
Free Radic Biol Med 2013;110:18826
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