R8781 Sigma


Ready Made Solution, 2.5 mg/mL in DMSO (2.74 mM), from Streptomyces hygroscopicus

Synonym: 23,27-Epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclohentriacontine solution



Related Categories Approved Therapeutics/Drug Candidates, Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, Pfizer Compounds,
Quality Level   PREMIUM
biological source   from Streptomyces hygroscopicus
sterility   0.2 μm filtered
assay   ≥95% (HPLC)
concentration   2.5 mg/mL in DMSO (2.74 mM)
antibiotic activity spectrum   fungi
originator   Pfizer
storage temp.   −20°C


Biochem/physiol Actions

Rapamycin is a macrocyclic triene antibiotic possessing potent immunosuppressant and anticancer activity. It forms a complex with FKBP12 that binds to and inhibits the molecular target of rapamycin (mTOR). mTOR is a member of the phosphoinositide kinase-related kinase (PIKK) family that enhances cellular proliferation via the phosphoinositol 3-kinase/Akt signaling pathway. Inhibition of this pathway by rapamycin blocks downstream elements that result in cell cycle arrest in G1. The effectors of mTOR action include 4EBP1 and S6K1.

Features and Benefits

This compound is featured on the Phosphoinositide Kinases page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

This compound was developed by Pfizer. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Protocols & Applications

Antibiotic Selector for application, solubility, solution stability, working concentration, and mode of action information

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Safety & Documentation

Safety Information

NA 1993 / PGIII
WGK Germany 
Flash Point(F) 
188.6 °F
Flash Point(C) 
87 °C


Certificate of Analysis

Certificate of Origin

Protocols & Articles


Discover Bioactive Small Molecules for Immunology Research

The immune system is a complex network to detect and defend against non-self pathogenic agents, such as disease-causing viruses, bacteria, and other microorganisms. Various signaling pathways contrib...
Keywords: Antibiotics, Antifungals, Antivirals, Apoptosis, Bioactive small molecules, Cell signaling, Diabetes, Diseases, Immunology, Inflammation

Phosphoinositide Kinases

The membranes of all metazoan cells contain a substantial amount of phosphatidylinositol (PtdIns) and at least seven phosphorylated PtdIns derivatives (PPIn) at 30- to 1000-fold lower concentrations....
Keywords: Cancer, Catalysis, Gene expression, Genetic, Growth factors, Phosphorylations

Peer-Reviewed Papers


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Rapamycin reverses cellular phenotypes and enhances mutant protein clearance in Hutchinson-Gilford Progeria Syndrome cells. Cao, K. et al. Sci. Transl. Med. 3, (2011)


Secretory phospholipase A2-IID is an effector molecule of CD4+CD25+ regulatory T cells. von Allmen CE, Schmitz N, Bauer M, et al. Proc. Natl. Acad. Sci. U. S. A. 106(28), 11673-8, (2009)


Hepatitis C virus present in the sera of infected patients interferes with the autophagic process of monocytes impairing their in-vitro differentiation into dendritic cells. Granato M, Lacconi V, Peddis M, et al. Biochim. Biophys. Acta 1843(7), 1348-55, (2014)

Neuropilin-1 expression on regulatory T cells enhances their interactions with dendritic cells during antigen recognition. Sarris M Immunity 28(3), 402-13, (2008)


A role for the NAD-dependent deacetylase Sirt1 in the regulation of autophagy Lombard, D.B., et al. Proc. Natl. Acad. Sci. U. S. A. 105, 3374-3379, (2008)


Passive immunization reduces behavioral and neuropathological deficits in an alpha-synuclein transgenic model of Lewy body disease. Masliah E, Rockenstein E, Mante M, et al. PLoS ONE 6(4), e19338, (2011)


EGFR signaling through an Akt-SREBP-1-dependent, rapamycin-resistant pathway sensitizes glioblastomas to antilipogenic therapy. Deliang Guo et al Sci. Signal. 2, ra82, (2010)


LKB1/KRAS mutant lung cancers constitute a genetic subset of NSCLC with increased sensitivity to MAPK and mTOR signalling inhibition. Mahoney CL Br. J. Cancer 100(2), 370-5, (2009)


Tuberous sclerosis complex and Myc coordinate the growth and division of Drosophila intestinal stem cells. Alla Amcheslavsky et al J. Cell Biol. 193, 695-710, (2011)


Cytoplasmic sequestration of p27 via AKT phosphorylation in renal cell carcinoma. Jinhee Kim et al Clin. Cancer Res. 15, 81-90, (2010)


Phosphorylation of eukaryotic translation initiation factor 2α coordinates rRNA transcription and translation inhibition during endoplasmic reticulum stress. Jenny B. DuRose et al Mol. Cell. Biol. 29, 4295-307, (2009)


Regulating amyloid precursor protein synthesis through an internal ribosomal entry site. Beaudoin ME Nucleic Acids Res. 36(21), 6835-47, (2008)


AMP-activated protein kinase is essential for survival in chronic hypoxia. Darrell R. Borger et al Biochem. Biophys. Res. Commun. 370, 230-4, (2008)


Metformin as adjunct antituberculosis therapy. Singhal A, Jie L, Kumar P, et al. Sci. Transl. Med. 6(263), 263ra159, (2014)


NuMA interacts with phosphoinositides and links the mitotic spindle with the plasma membrane. Kotak S, Busso C, and Gönczy P EMBO J. 33(16), 1815-30, (2014)


Itraconazole suppresses the growth of glioblastoma through induction of autophagy: involvement of abnormal cholesterol trafficking. Liu R, Li J, Zhang T, et al. Autophagy 10(7), 1241-55, (2014)


Autophagy-inducing peptides from mammalian VSV and fish VHSV rhabdoviral G glycoproteins (G) as models for the development of new therapeutic molecules. García-Valtanen P, Ortega-Villaizán Mdel M, Martínez-López A, et al. Autophagy 10(9), 1666-80, (2014)


Merck 14,8114

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