Antibiotic with immunosuppressant and anti-cancer properties
Commonly used to study autophagy in a variety of cells
Highly cited
Rapamycin is a macrocyclic-triene antibiotic with potent immunosuppressant activity. Rapamycin forms a complex with FKBP12 that binds to an effector, thus inhibiting IL-2 and other growth promoting lymphokines. The effectors were identified as FRAP (FKBP12 rapamycin-associated protein) and RAFT1 (rapamycin and KFBP12 target). Rapamycin/FKBP complex does not inhibit FRAP PI 4-kinase activity, but does inhibit FRAP autophosphorylation. Rapamycin induces inhibition of p70s6k, p33cdk2 and p34cdc2. Rapamycin selectively blocks signaling leading to the activation of p70/85 S6 kinase. Rapamycin complexed with FKBP12 binds to and inhibits the activity of the mammalian target of rapamycin (mTOR) complex 1 (mTORC1). Rapamycin can inhibit cell growth, enhance apoptosis, and activates autophagy in a variety of cell types.
Product Details
Alternative Name:
Sirolimus, AY-22,989, RAPA, Rapamune
Formula:
C51H79NO13
MW:
914.2
Source:
Isolated from Streptomyces hygroscopus
CAS:
53123-88-9
MI:
14: 8114
RTECS:
VE6250000
Purity:
≥98% (HPLC)
Appearance:
Off-white or yellow solid.
Solubility:
Soluble in chloroform, DMSO (25mg/ml), or 100% methanol.
Shipping:
Ambient Temperature
Long Term Storage:
-20°C
Use/Stability:
Store, as supplied, at -20°C for up to 1 year. Store solutions at -20°C for up to 3 months.
Technical Info/Product Notes:
Replacement for ADI-HPK-109.
Regulatory Status:
RUO - Research Use Only
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Product Literature References
Impaired degradation of YAP1 and IL6ST by chaperone-mediated autophagy promotes proliferation and migration of normal and hepatocellular carcinoma cells: E. Desideri, et al.; Autophagy 19, 152 (2023), Abstract;
Streptococcal arginine deiminase regulates endothelial inflammation, mTOR pathway and autophagy: J.T. Mammedova, et al.; Immunobiology 228, 152344 (2023), Abstract;
An amino acid-defined diet impairs tumour growth in mice by promoting endoplasmic reticulum stress and mTOR inhibition: M. Ragni, et al.; Mol. Metab. 60, 101478 (2022), Abstract;
Fluorescence imaging detection of nanodomain redox signaling events at organellar contacts: D.M. Booth, et al.; STAR Protoc. 3, 101119 (2022), Abstract; Full Text
Ipecac root extracts and isolated circular peptides differentially suppress inflammatory immune response characterised by proliferation, activation and degranulation capacity of human lymphocytes in vitro: C.M. Falanga, et al.; Biomed. Pharmacother. 152, 113120 (2022), Abstract;
Microtubule organizing centers regulate spindle positioning in mouse oocytes: D. Londono-Vasquez, et al.; Dev. Cell 57, 197 (2022), Abstract;
NMD is required for timely cell fate transitions by fine-tuning gene expression and regulating translation: M. Huth, et al.; Genes Dev. 36, 348 (2022), Abstract; Full Text
RAPIDS, a method for sub-compartmental identification of protein interactomes: C. James, et al.; Methods Enzymol. 675, 109 (2022), Abstract;
Rgs16 promotes antitumor CD8+ T cell exhaustion: N. Weisshaar, et al.; Sci. Immunol. 7, eabh1873 (2022), Abstract;
The autophagy protein Pacer positively regulates the therapeutic potential of mesenchymal stem cells in a mouse model of DSS-induced colitis: C. Bergmann, et al.; Cells 11, 1503 (2022), Abstract; Full Text
The methyltransferase enzymes KMT2D, SETD1B, and ASH1L are key mediators of both metabolic and epigenetic changes during cellular senescence: T. Nacarelli, et al.; Mol. Biol. Cell 33, ar36 (2022), Abstract;
Autophagy-Associated IL-15 Production Is Involved in the Pathogenesis of Leprosy Type 1 Reaction: B.J.A. Silva, et al.; Cells 10, 2215 (2021), Abstract;
Carbon Monoxide Releasing Molecule-3 Enhances Heme Oxygenase-1 Induction via ROS-Dependent FoxO1 and Nrf2 in Brain Astrocytes: C. C. Lin, et al.; Oxid. Med. Cell. Longev. 2021, 5521196 (2021), Abstract;
Distinct alpha-Synuclein species induced by seeding are selectively cleared by the Lysosome or the Proteasome in neuronally differentiated SH-SY5Y cells: M. Pantazopoulou, et al.; J. Neurochem. 156, 880 (2021), Abstract;
Mitochondrial and Clearance Impairment in p.D620N VPS35 Patient-Derived Neurons: Z. Hanss, et al.; Mov. Disord. 36, 704 (2021), Application(s): Treatment of iPSCs-derived neurons, Abstract; Full Text
Oxidative bursts of single mitochondria mediate retrograde signaling toward the ER: D. Booth, et al.; Mol. Cell 81, 3866 (2021), Abstract; Full Text
Raft-like lipid microdomains drive autophagy initiation via AMBRA1-ERLIN1 molecular association within MAMs: V. Manganelli, et al.; Autophagy 17, 2528 (2021), Abstract; Full Text
Receptor-mediated endocytosis 8 (RME-8)/DNAJC13 is a novel positive modulator of autophagy and stabilizes cellular protein homeostasis: A. Besemer, et al.; Cell. Mol. Life Sci. 78, 645 (2021), Abstract; Full Text
The selective degradation of sirtuins via macroautophagy in the MPP+ model of Parkinson’s disease is promoted by conserved oxidation sites: M.W. Baeken, et al.; Cell Death Discov. 7, 286 (2021), Abstract;
Trehalose causes low-grade lysosomal stress to activate TFEB and the autophagy-lysosome biogenesis response: S.J. Jeong, et al.; Autophagy 17, 3740 (2021), Abstract; Full Text
Incorporation of docetaxel and thymoquinone in borage nanoemulsion potentiates their antineoplastic activity in breast cancer cells: M.H. Alkhatib, et al.; Sci. Rep. 10, 18124 (2020), Abstract; Full Text
Lipid-droplet formation drives pathogenic group 2 innate lymphoid cells in airway inflammation: F. Karagiannis, et al.; Immunity 52, 620 (2020), Abstract;
Lymphatics in bone arise from pre-existing lymphatics: M. Monroy, et al.; Development 147, dev184291 (2020), Abstract; Full Text
Pharmacological inhibition of mTORC1 increases CCKBR-specific tumor uptake of radiolabeled minigastrin analogue [ 177 Lu]Lu-PP-F11N: M. Grzmil, et al.; Theranostics 10, 10861 (2020), Abstract; Full Text
Prolyl oligopeptidase inhibition activates autophagy via protein phosphatase 2A: R. Svarcbahs, et al.; Pharmacol. Res. 151, 104558 (2020), Abstract;
RAB18 loss interferes with lipid droplet catabolism and provokes autophagy network adaptations: F. Bekbulat, et al.; J. Mol. Biol. 432, 1216 (2020), Abstract;
Rejection of xenogeneic porcine islets in humanized mice is characterized by graft-infiltrating Th17 cells and activated B cells: F.T. Lee, et al.; Am. J. Transplant. 20, 1538 (2020), Abstract; Full Text
Tanycytic TSPO inhibition induces lipophagy to regulate lipid metabolism and improve energy balance: S. Kim, et al.; Autophagy 16, 1200 (2020), Abstract; Full Text
The effect of prolyl oligopeptidase inhibitors on alpha-synuclein aggregation and autophagy cannot be predicted by their inhibitory efficacy: T. Kilpelainen, et al.; Biomed. Pharmacother. 128, 110253 (2020), Abstract;
CSB promoter downregulation via histone H3 hypoacetylation is an early determinant of replicative senescence: C. Crochemore, et al.; Nat. Commun. 10, 5576 (2019), Abstract; Full Text
Effect of selective serotonin (5-HT)2B receptor agonist BW723C86 on epidermal growth factor/transforming growth factor-α receptor tyrosine kinase and ribosomal p70 S6 kinase activities in primary cultures of adult rat hepatocytes: K. Naito, et al.; Biol. Pharm. Bull. 42, 631 (2019), Application(s): used w. adult rat liver hepatocytes, Abstract; Full Text
Enhanced autophagic-lysosomal activity and increased BAG3-mediated selective macroautophagy as adaptive response of neuronal cells to chronic oxidative stress: D. Chakraborty, et al.; Redox Biol. 24, 101181 (2019), Abstract; Full Text
Fas‐apoptotic inhibitory molecule 2 localizes to the lysosome and facilitates autophagosome‐lysosome fusion through the LC3 interaction region motif–dependent interaction with LC3: C.J. Hong, et al.; FASEB J. 34, 161 (2019), Abstract; Full Text
Linagliptin inhibits high glucose-induced transdifferentiation of hypertrophic scar-derived fibroblasts to myofibroblasts via IGF/Akt/mTOR signalling pathway: Y. Li, et al.; Exp. Dermatol. 28, 19 (2019), Abstract;
Loss of neurological disease HSAN-I-associated gene SPTLC2 impairs CD8+ T cell responses to infection by inhibiting T cell metabolic fitness: J. Wu, et al.; Immunity 50, 1218 (2019), Abstract; Full Text
Nemo-like kinase drives Foxp3 stability and is critical for maintenance of immune tolerance by regulatory T cells: V. Fleskens, et al.; Cell Rep. 26, 3600 (2019), Abstract; Full Text
Network approach identifies Pacer as an autophagy protein involved in ALS pathogenesis: S. Beltran, et al.; Mol. Neurodegener. 14, 14 (2019), Abstract; Full Text
Promoter distortion and opening in the RNA polymerase II cleft: C. Dienemann, et al.; Mol. Cell 73, 97 (2019), Abstract;
Somatic activating mutations in PIK3CA cause generalized lymphatic anomaly: L. Rodriguez-Laguna, et al.; J. Exp. Med. 216, 407 (2019), Abstract; Full Text
TLR4 (toll-like receptor 4) activation suppresses autophagy through inhibition of FOXO3 and impairs phagocytic capacity of microglia: J.W. Lee, et al.; Autophagy 15, 753 (2019), Abstract; Full Text
Topical rapamycin reduces markers of senescence and aging in human skin: an exploratory, prospective, randomized trial: C. Chung, et al.; Geroscience 41, 861 (2019), Abstract; Full Text
Locally Produced IGF-1 Promotes Hypertrophy of the Ligamentum Flavum via the mTORC1 Signaling Pathway: B. Yan, et al.; Cell. Physiol. Biochem. 48, 293 (2018), Abstract; Full Text
Loperamide, pimozide, and STF-62247 trigger autophagy-dependent cell death in glioblastoma cells: S. Zielke, et al.; Cell Death Dis. 9, 994 (2018), Abstract; Full Text
LXRɑ participates in the mTOR/S6K1/SREBP-1c signaling pathway during sodium palmitate-induced lipogenesis in HepG2 cells: Y. Zhou, et al.; Nutr. Metab. (Lond.) 15, 31 (2018), Abstract; Full Text
Peripheral Synthesis of an Atypical Protein Kinase C Mediates the Enhancement of Excitability and the Development of Mechanical Hyperalgesia Produced by Nerve Growth Factor: J. Kays, et al.; Neuroscience 371, 420 (2018), Abstract;
The RAB GTPase RAB18 modulates macroautophagy and proteostasis: A. Feldmann, et al.; Biochem. Biophys. Res. Commun. 486, 738 (2017), Abstract;
An inhibitor of HIV-1 protease modulates constitutive eIF2α dephosphorylation to trigger a specific integrated stress response: A. De Gassart, et al.; PNAS 113, E117 (2016), Application(s): Cell culture, Abstract; Full Text
IL-2, IL-4, IFN-γ or TNF-α enhances BAFF-stimulated cell viability and survival by activating Erk1/2 and S6K1 pathways in neoplastic B-lymphoid cells: L. Gui, et al.; Cytokine 84, 37 (2016), Application(s): Cell culture, Abstract;
Lutein Attenuates Both Apoptosis and Autophagy upon Cobalt (II) Chloride-Induced Hypoxia in Rat Műller Cells: F.K. Fung, et al.; PLoS One 11, e0167828 (2016), Abstract;
Rapamycin ameliorates cadmium-induced activation of MAPK pathway and neuronal apoptosis by preventing mitochondrial ROS inactivation of PP2A: C. Xu, et al.; Neuropharmacology 105, 270 (2016), Application(s): Cell culture, Abstract;
Serotonin 5-HT2B Receptor-Stimulated DNA Synthesis and Proliferation Are Mediated by Autocrine Secretion of Transforming Growth Factor-α in Primary Cultures of Adult Rat Hepatocytes: K. Naito, et al.; Biol. Pharm. Bull. 39, 570 (2016), Application(s): Effects of Various Doses of Selective 5-HT2 Receptor Antagonists on DNA Synthesis and Proliferation in Hepatocytes, Abstract; Full Text
Sustained activation of mTORC1 in macrophages increases AMPKα-dependent autophagy to maintain cellular homeostasis: H. Pan, et al.; BMC Biochem. 17, 14 (2016), Application(s): Immunofluorescence microscopy - involvement in cell cycle processes, Abstract; Full Text
Transforming Growth Factor-β1 Increases DNA Methyltransferase 1 and -3a Expression Through Distinct Post-transcriptional Mechanisms in Lung Fibroblasts: H.B. Koh, et al.; J. Biol. Chem. 291, 19287 (2016), Application(s): Cell culture; mTOR inhibitor, normal primary human lung fibroblasts, Abstract; Full Text
Cinnamic aldehyde suppresses hypoxia-induced angiogenesis via inhibition of hypoxia-inducible factor-1α expression during tumor progression: W.Y. Bae, et al.; Biochem. Pharmacol. 98, 41 (2015), Application(s): Cell culture , Abstract;
Glutamate Stimulates Local Protein Synthesis in the Axons of Rat Cortical Neurons by Activating AMPA Receptors and Metabotropic Glutamate Receptors: W.L. Hsu, et al.; J. Biol. Chem. 390, 20748 (2015), Application(s): Cell Culture, Abstract; Full Text
ILT4 drives B7-H3 expression via PI3K/AKT/mTOR signalling and ILT4/B7-H3 co-expression correlates with poor prognosis in non-small cell lung cancer: P. Zhang, et al.; FEBS Lett. 589, 2248 (2015), Application(s): Cell Culture, Abstract;
Induction of apoptosis and autophagy via sirtuin1- and PI3K/Akt/mTOR-mediated pathways by plumbagin in human prostate cancer cells: Z.W. Zhou, et al.; Drug Des. Devel. Ther. 9, 1511 (2015), Application(s): Cell Culture, Assay, Abstract; Full Text
Regulation of autophagy by coordinated action of mTORC1 and protein phosphatase 2A: P.M. Wong, et al.; Nat. Commun. 6, 8048 (2015), Application(s): Cell Culture, Abstract; Full Text
Coxiella burnetii Type IV Secretion-Dependent Recruitment of Macrophage Autophagosomes: C.G. Winchell, et al.; Infect. Immun. 82, 2229 (2014), Application(s): Role of the T4SS in mediating PV interactions with autophagosomes, Abstract;
Anti-tumor efficacy of a hepatocellular carcinoma vaccine based on dendritic cells combined with tumor-derived autophagosomes in murine models: S. Su, et al.; Asian Pac. J. Cancer Prev. 14, 3109 (2013), Application(s): WB, Fluorescence Microscopy, PCR, Abstract; Full Text
Dealcoholated red wine induces autophagic and apoptotic cell death in an osteosarcoma cell line: I. Tedesco, et al.; Food Chem. Toxicol. 60, 377 (2013), Application(s): WB, Fluorescence Microscopy, Abstract;
Direct imaging reveals stable, micrometer-scale lipid domains that segregate proteins in live cells: A. Toulmay; J. Cell Biol. 202, 35 (2013), Application(s): Fluorescence Microscopy, Abstract; Full Text
Rapamycin decreases tau phosphorylation at Ser214 through regulation of cAMP-dependent kinase: Y. Liu, et al.; Neurochem. Int. 62, 458 (2013), Application(s): WB, IP, Confocal microscopy, Abstract;
Reduced mammalian target of rapamycin activity facilitates mitochondrial retrograde signaling and increases life span in normal human fibroblasts: C. Lerner, et al.; Aging Cell 12, 966 (2013), Application(s): WB, Abstract; Full Text
Remarkable inhibition of mTOR signaling by the combination of rapamycin and 1,4-phenylenebis(methylene)selenocyanate in human prostate cancer cells: N.D. Facompre, et al.; Int. J. Cancer 131, 2134 (2013), Application(s): WB, IP, Abstract; Full Text
Preclinical modeling of combined phosphatidylinositol-3-kinase inhibition with endocrine therapy for estrogen receptor-positive breast cancer: C.G. Sanchez, et al.; Breast Cancer Res. 13, R21 (2011), Application(s): WB, Abstract; Full Text
Long-Term IGF-I Exposure Decreases Autophagy and Cell Viability: A. Bitto, et al.; PloS One 5, e12592 (2010), Application(s): WB, Fluorescence Microscopy, Electron Microscopy , Abstract; Full Text
mTOR inhibitors (rapamycin and its derivatives) and nitrogen containing bisphosphonates: bi-functional compounds for the treatment of bone tumours: B. Ory, et al.; Curr. Med. Chem. 14, 1381 (2007), Review, Abstract;
Rapamycin causes poorly reversible inhibition of mTOR and induces p53- independent apoptosis in human rhabdomyosarcoma cells: H. Hosoi, et al.; Cancer Res. 59, 886 (1999), Abstract;
Rapamycin inhibition of the G1 to S transition is mediated by effects on cyclin D1 mRNA and protein stability: S. Hashemolhosseini, et al.; J. Biol. Chem. 273, 14424 (1998), Abstract; Full Text
Rapamycin and p53 act on different pathways to induce G1 arrest in mammalian cells: S.M. Metcalfe, et al.; Oncogene 15, 1635 (1997), Abstract;
Rapamycin potentiates dexamethasone-induced apoptosis and inhibits JNK activity in lymphoblastoid cells: T. Ishizuka, et al.; BBRC 230, 386 (1997), Abstract;
Structure of the FKBP12-rapamycin complex interacting with the binding domain of human FRAP: J. Choi et al.; Science 273, 239 (1996), Abstract;
Control of p70 s6 kinase by kinase activity of FRAP in vivo: E.J. Brown et al.; Nature 377, 441 (1995), Abstract;
Rapamycin enhances apoptosis and increases sensitivity to cisplatin in vitro: Y. Shi, et al.; Cancer Res. 55, 1982 (1995), Abstract;
Rapamycin, a potent immunosuppressive drug, causes programmed cell death in B lymphoma cells: S. Muthukkumar, et al.; Transplantation 60, 264 (1995), Abstract;
The rapamycin and FKBP12 target (RAFT) displays phosphatidylinositol 4-kinase activity: D.M. Sabatini et al.; J. Biol. Chem. 270, 20875 (1995), Abstract;
A mammalian protein targeted by G1-arresting rapamycin-receptor complex: E.J. Brown, et al.; Nature 369, 756 (1994), Abstract;
RAFT1: a mammalian protein that binds to FKBP12 in a rapamycin- dependent fashion and is homologous to yeast TORs: D.M. Sabatini, et al.; Cell 78, 35 (1994), Abstract;
Dissociation of pp70 ribosomal protein S6 kinase from insulin-stimulated glucose transport in 3T3-L1 adipocytes: D.C. Fingar et al.; J. Biol. Chem. 268, 3005 (1993), Abstract;
Rapamycin inhibition of interleukin-2-dependent p33cdk2 and p34cdc2 kinase activation in T lymphocytes: W.G. Morice, et al.; J. Biol. Chem. 268, 22737 (1993), Abstract; Full Text
Rapamycin-induced inhibition of p34cdc2 kinase activation is associated with G1/S-phase growth arrest in T lymphocytes: W.G. Morice et al.; J. Biol. Chem. 268, 3734 (1993), Abstract;
Rapamycin: in vitro profile of a new immunosuppressive macrolide: S.N. Sehgal & C.C. Bansback; Ann. N. Y. Acad. Sci. 685, 58 (1993), Abstract;
Rapamycin-FKBP specifically blocks growth-dependent activation of and signaling by the 70 kd S6 protein kinases: J. Chung et al.; Cell 69, 1227 (1992), Abstract;
Rapamycin-induced inhibition of the 70-kilodalton S6 protein kinase: D.J. Price, et al.; Science 257, 973 (1992), Abstract;
FK506 and rapamycin: novel pharmacological probes of the immune response: J.Y. Chang et al.; Trends Pharmacol. Sci. 12, 218 (1991), Abstract;
Inhibition of T and B lymphocyte proliferation by rapamycin: J.E. Kay et al.; Immunology 72, 544 (1991), Abstract;
Targets for cell cycle arrest by the immunosuppressant rapamycin in yeast: J. Heitman et al.; J. Heitman et al. 253, 905 (1991), Abstract;
Rapamycin (AY-22,989), a new antifungal antibiotic. I. Taxonomy of the producing streptomycete and isolation of the active principle: C. Vezina, et al.; J. Antibiot. (Tokyo) 28, 721 (1975), Abstract;
Rapamycin (AY-22,989), a new antifungal antibiotic. II. Fermentation, isolation and characterization: S.N. Sehgal, et al.; J. Antibiot. (Tokyo) 28, 727 (1975), Abstract;
