Chemical Name: (3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,10,12,13,14,21,22,23,24,25,26,27,32,33,34,34a-Hexadecahydro-9,27-dihydroxy-3-[(1R)-2-[(1S,3R,4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylethyl]-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-23,27-epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclohentriacontine-1,5,11,28,29(4H,6H,31H)-pentone
Biological ActivityAntifungal and immunosuppressant. Specific inhibitor of mTOR (mammalian target of Rapamycin). Complexes with FKBP-12 and binds mTOR inhibiting its activity. Inhibits interleukin-2-induced phosphorylation and activation of p70 S6 kinase. Induces autophagy in yeast and mammalian cell lines. Drives hPSC differentiation to mesendoderm and blood progenitor cells. Also used as a chemical dimerizer; rapamycin and GA3-AM (Cat. No. 5407) chemically inducible dimerization systems are orthogonal.
External Portal InformationChemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of Rapamycin is reviewed on the chemical probes website.
The technical data provided above is for guidance only.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Pharmacological modulation of autophagy: therapeutic potential and persisting obstacles.
Galluzzi et al.
Rapamycin, a specific inhibitor of the mammalian target of rapamycin, suppresses lymphangiogenesis and lymphatic metastasis.
Kobayashi et al.
Cancer Sci., 2007;98:726
Rapamycins: mechanism of action and cellular resistance.
Huang et al.
Cancer Biol.Ther., 2003;2:221
Rapamycin selectively inhibits interleukin-2 activation of p70 S6 kinase.
Kuo et al.
A multi-lineage screen reveals mTORC1 inhibition enhances human pluripotent stem cell mesendoderm and blood progenitor production.
Nazareth et al.
Stem Cell Reports, 2016;6:679
Rapid and orthogonal logic gating with a gibberellin-induced dimerization system
Miyamoto et al.
Citations for Rapamycin
The citations listed below are publications that use Tocris products. Selected citations for Rapamycin include:
42 Citations: Showing 1 - 10
Eicosapentaenoic acid attenuates dexamethasome-induced apoptosis by inducing adaptive autophagy via GPR120 in murine bone marrow-derived mesenchymal stem cells.
Authors: Gao Et al.
Cell Death Dis 2016;7:e2235
Vitamin C alleviates aging defects in a stem cell model for Werner syndrome.
Authors: Li Et al.
Protein Cell 2016;7:478
Diagnostic and clinical relevance of the autophago-lysosomal network in human gliomas.
Authors: Jennewein Et al.
Activation of the Mammalian Target of Rapamycin in the Rostral Ventromedial Medulla Contributes to the Maintenance of Nerve Injury-Induced Neuropathic Pain in Rat.
Authors: Wang Et al.
Neural Plast 2016;2015:394820
Bone morphogenetic protein dominantly suppresses epidermal growth factor-induced proliferative expansion of adult forebrain neural precursors.
Authors: Joppé Et al.
Nat Cell Biol 2015;9:407
Modulation of BK channels contributes to activity-dependent increase of excitability through MTORC1 activity in CA1 pyramidal cells of mouse hippocampus.
Authors: Springer Et al.
Mol Biol Cell 2015;8:451
PAK2 is an effector of TSC1/2 signaling independent of mTOR and a potential therapeutic target for Tuberous Sclerosis Complex.
Authors: Alves Et al.
Front Cell Neurosci 2015;5:14534
GSK3-mediated raptor phosphorylation supports amino-acid-dependent mTORC1-directed signalling.
Authors: Stretton Et al.
Front Neurosci 2015;470:207
A novel MEK-ERK-AMPK signaling axis controls chemokine receptor CCR7-dependent survival in human mature dendritic cells.
Authors: López-Cotarelo Et al.
Mol Brain 2015;290:827
Inflammation-induced desmoglein-2 ectodomain shedding compromises the mucosal barrier.
Authors: Kamekura Et al.
Biochem J 2015;26:3165
Docosahexaenoic Acid Induces Cell Death in Human Non-Small Cell Lung Cancer Cells by Repressing mTOR via AMPK Activation and PI3K/Akt Inhibition.
Authors: Kim Et al.
Biomed Res Int 2015;2015:239764
Mechanistic Target of Rapamycin Complex 1/S6 Kinase 1 Signals Influence T Cell Activation Independently of Ribosomal Protein S6 Phosphorylation.
Authors: Salmond Et al.
J Immunol 2015;195:4615
Cardiolipin remodeling by TAZ/tafazzin is selectively required for the initiation of mitophagy.
Authors: Hsu Et al.
Anti-Tumor Activity of Yuanhuacine by Regulating AMPK/mTOR Signaling Pathway and Actin Cytoskeleton Organization in Non-Small Cell Lung Cancer Cells.
Authors: Kang Et al.
PLoS One 2015;10:e0144368
SILAC-Based Mass Spectrometry Analysis Reveals That Epibrassinolide Induces Apoptosis via Activating Endoplasmic Reticulum Stress in Prostate Cancer Cells.
Authors: Obakan Et al.
PLoS One 2015;10:e0135788
SynGAP regulates protein synthesis and homeostatic synaptic plasticity in developing cortical networks.
Authors: Wang Et al.
PLoS One 2014;8:e83941
Angiogenic growth factors augment K-Cl cotransporter expression in erythroid cells via hypoxia-inducible factor-1α.
Authors: Gonsalves Et al.
Am J Hematol 2014;89:273
West nile virus-induced activation of mammalian target of rapamycin complex 1 supports viral growth and viral protein expression.
Authors: Shives Et al.
J Virol 2014;88:9458
Interaction of mTOR and Erk1/2 signaling to regulate oligodendrocyte differentiation.
Authors: Dai Et al.
Long-term potentiation can be induced in the CA1 region of hippocampus in the absence of αCaMKII T286-autophosphorylation.
Authors: Villers Et al.
Learn Mem 2014;21:616
A genetic screen identifies an LKB1-MARK signalling axis controlling the Hippo-YAP pathway.
Authors: Mohseni Et al.
J Virol 2014;16:108
Adaptation to mTOR kinase inhibitors by amplification of eIF4E to maintain cap-dependent translation.
Authors: Cope Et al.
J Cell Sci 2014;127:788
Parallel measurement of dynamic changes in translation rates in single cells.
Authors: Han Et al.
Nat Methods 2014;11:86
Inhibition of autophagy as a new means of improving chemotherapy efficiency in high-LC3B triple-negative breast cancers.
Authors: Lefort Et al.
Suppression of MAPK/JNK-MTORC1 signaling leads to premature loss of organelles and nuclei by autophagy during terminal differentiation of lens fiber cells.
Authors: Basu Et al.
Activation of mammalian target of rapamycin mediates rat pain-related responses induced by BmK I, a sodium channel-specific modulator.
Authors: Jiang Et al.
Mol Pain 2013;9:50
Herpes simplex virus 2 (HSV-2) prevents dendritic cell maturation, induces apoptosis, and triggers release of proinflammatory cytokines: potential links to HSV-HIV synergy.
Authors: Stefanidou Et al.
J Biol Chem 2013;87:1443
Neuroprotection through excitability and mTOR required in ALS motoneurons to delay disease and extend survival.
Authors: Saxena Et al.
Post-transcriptional regulation of GABAB receptor and GIRK1 channels by Nogo receptor 1.
Authors: Murthy Et al.
Cereb Cortex 2013;6:30
Asymmetrical synaptic cooperation between cortical and thalamic inputs to the amygdale.
Identification of repurposed small molecule drugs for chordoma therapy.
Authors: Xia Et al.
Cancer Biol Ther 2013;14:638
Ceramide 1-phosphate stimulates proliferation of C2C12 myoblasts.
Authors: Gangoiti Et al.
Immunohistochemical detection of cytoplasmic LC3 puncta in human cancer specimens.
Authors: Ladoire Et al.
Fucoidan from seaweed Fucus vesiculosus inhibits migration and invasion of human lung cancer cell via PI3K-Akt-mTOR pathways.
Authors: Lee Et al.
PLoS One 2012;7:e50624
Insulin-like growth factors promote vasculogenesis in embryonic stem cells.
Authors: Piecewicz Et al.
PLoS One 2012;7:e32191
Passenger deletions generate therapeutic vulnerabilities in cancer.
Authors: Muller Et al.
Erlotinib antagonizes ABC transporters in acute myeloid leukemia.
Authors: Lainey Et al.
Cell Cycle 2012;11:4079
Pro-autophagic polyphenols reduce the acetylation of cytoplasmic proteins.
Authors: Pietrocola Et al.
Cell Cycle 2012;11:3851
Docosahexaenoic acid induces autophagy through p53/AMPK/mTOR signaling and promotes apoptosis in human cancer cells harboring wild-type p53.
Authors: Jing Et al.
Sci Rep 2011;7:1348
The angiogenic factor angiopoietin-1 is a proneurogenic peptide on subventricular zone stem/progenitor cells.
Authors: Rosa Et al.
J Neurosci 2010;30:4573
BC1 regulation of metabotropic glutamate receptor-mediated neuronal excitability.
Authors: Zhong Et al.
J Neurosci 2009;29:9977
Dysregulated metabotropic glutamate receptor-dependent translation of AMPA receptor and postsynaptic density-95 mRNAs at synapses in a mouse model of fragile X syndrome.
Authors: Muddashetty Et al.
J Neurosci 2007;27:5338
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