Home PI3K/Akt/mTOR mTOR inhibitor - Autophagy activator - Antineoplastic and Immunosuppressive Antibiotics chemical Rapamycin For research use only.

Rapamycin

Synonyms: AY-22989, NSC-2260804

Rapamycin is a specific mTOR inhibitor with IC50 of ~0.1 nM in HEK293 cells.Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator and an immunosuppressant.

Rapamycin Chemical Structure

Rapamycin Chemical Structure

CAS No. 53123-88-9

Purity & Quality Control

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Rapamycin Related Products

Signaling Pathway

mTOR Signaling Pathways

mTOR Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
COS7 cells expressing EGFP-LC3 Autophagy Assay 0.2 μM 24 h DMSO Induces autophagy 18391949
H4 Function Assay 0.2 μM 24 h DMSO Increases the ratio of light chain 3 subunit 2 to light chain 3 subunit 1 in human H4 cells 18024584
COS7 cells expressing EGFP-HDQ74/rheb Autophagy Assay 0.2 μM 24 h DMSO Induces autophagy 18391949
PBMC Function Assay 1 nM 14 d DMSO Reduces CCR5 density 17485501
HEK293T Antiviral Assay 1 nM 4 d DMSO Induces antiviral activity against HIV1 X4 with EC50 of 0.3 nM 17485501
U87MG Kinase Assay 1 μM 6 h DMSO Potently inhibits mTOR-mediated S6 phosphorylation 19848404
cells from the thymus of normal BALB/c mice Growth Inhibition Assay 10 nM 72 h DMSO Inhibits lymphoproliferation (LAF) with IC50 of 3 nM 10021948
PC3 Growth Inhibition Assay 1.5 μM 1 h DMSO Induces antiproliferative activity against human PC3 cells with IC50 of <10 nM 21978683
HT-29 Cytotoxic Assay 10 nM 72 h DMSO Potentiates digitoxin-induced cytotoxicity 24900873
Drosophila melanogaster S2 cells transfected with N-luc and C-luc Function Assay 100 nM 4 h DMSO Induces luciferase protein trans-splicing in Drosophila melanogaster S2 cells transfected with N-luc and C-luc 17128262
SYF Function Assay 100 nM 24 h DMSO Induces FRB-FKBP complex interaction 17563385
HEK293 Function Assay 100 nM 8 h DMSO Inhibits TPA-induced degradation of Pdcd4 with EC50 of 50 nM 21539301
HeLa Function Assay 100 nM 36 h DMSO Induces FRB K2095P, T2098L, W2101F mutant-ubiquitinC interaction 17563385
BT-20 Kinase Assay 20 μM DMSO Does not inhibit mTORC2 dependent pAkT S473 phosphorylation 21353551
PC3 Kinase Assay 100 nM 1 h DMSO Potently inhibits mTOR-mediated S6 phosphorylation with IC50 of <10 nM. 21978683
Human mixed lymphocyte Growth Inhibition Assay 5 nM DMSO IC50=1.6 nM. 16185865
MCF-7 Autophagy Assay 30 nM 4 h DMSO Induces autophagy 20028134
Lewis rat lymph node cells Growth Inhibition Assay 5 μM DMSO IC50=2.6 μM 16185865
HEK293 cells Kinase Assay 50 nM 45 min DMSO Inhibits mTOR kinase activity with IC50 of 0.1 nM 17350953
U937 Antibacterial Assay 50 μM 48 h DMSO Induces antibacterial activity against wild type Legionella pneumophila Philadelphia-1 JR32 in U937 cells 21142106
Click to View More Cell Line Experimental Data

Biological Activity

Description Rapamycin is a specific mTOR inhibitor with IC50 of ~0.1 nM in HEK293 cells.Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator and an immunosuppressant.
Targets
mTOR [1]
(HEK293 cells)
~0.1 nM
In vitro
In vitro

Rapamycin inhibits endogenous mTOR activity in HEK293 cells with IC50 of ~0.1 nM, more potently than iRap and AP21967 with IC50 of ~5 nM and ~10 nM, respectively. [1] In Saccharomyces cerevisiae, Rapamycin treatment induces a severe G1/S cell cycle arrest and inhibition of translation initiation to levels below 20% of control. [2] Rapamycin significantly inhibits the cell viability of T98G and U87-MG in a dose-dependent manner with IC50 of 2 nM and 1 μM, respectively, while displaying little activity against U373-MG cells with IC50 of >25 μM despite the similar extent of the inhibition of mTOR signaling. Rapamycin (100 nM) induces G1 arrest and autophagy but not apoptosis in Rapamycin-sensitive U87-MG and T98G cells by inhibiting the function of mTOR. [3]
Kinase Assay Immunoblotting for the mTOR kinase assay
HEK293 cells are plated at 2-2.5×105 cells/well of a 12-well plate and serum-starved for 24 hours in DMEM. Cells are treated with increasing concentrations of Rapamycin (0.05-50 nM) for 15 minutes at 37 °C. Serum is added to a final concentration of 20% for 30 minutes at 37 °C. Cells are lysed, and cell lysates are separated by SDS-PAGE. Resolved proteins are transferred to a polyvinylidene difluoride membrane and immunoblotted with a phosphospecific primary antibody against Thr-389 of p70 S6 kinase. Data are analyzed using ImageQuant and KaleidaGr
Cell Research Cell lines U87-MG, T98G, and U373-MG
Concentrations Dissolved in DMSO, final concentrations ~25 μM
Incubation Time 72 hours
Method

Cells are exposed to various concentrations of Rapamycin for 72 hours. For the assessment of cell viability, cells are collected by trypsinization, stained with trypan blue, and the viable cells in each well are counted. For the determination of cell cycle, cells are trypsinized, fixed with 70% ethanol, and stained with propidium iodide using a flow cytometry reagent set. Samples are analyzed for DNA content using a FACScan flow cytometer and CellQuest software. For apoptosis detection, cells are stained with the terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling (TUNEL) technique using an ApopTag apoptosis detection kit. To detect the development of acidic vesicular organelles (AVO), cells are stained with acridine orange (1 μg/mL) for 15 minutes, and examined under a fluorescence microscope. To quantify the development of AVOs, cells are stained with acridine orange (1 μg/mL) for 15 minutes, removed from the plate with trypsin-EDTA, and analyzed using the FACScan flow cytometer and CellQuest software. To analyze the autophagic process, cells are incubated for 10 minutes with 0.05 mM monodansylcadaverine at 37 °C and are then observed under a fluorescence microscope.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-mTOR(S2448)/mTOR 23991038
Growth inhibition assay Cell proliferation 30393233
Histomorphology Haematoxylin & Eosin 28418837
Immunofluorescence NeuN p62/Beclin 28418837
ELISA Type III collagen/Fibronectin 23364979
In Vivo
In vivo

Treatment with Rapamycin in vivo specifically blocks targets known to be downstream of mTOR such as the phosphorylation and activation of p70S6K and the release of inhibition of eIF4E by PHAS-1/4E-BP1, leading to complete blockage of the hypertrophic increases in plantaris muscle weight and fibre size. [4] Short-term Rapamycin treatment, even at the lowest dose of 0.16 mg/kg, produces profound inhibition of p70S6K activity, which correlates with increased tumor cell death and necrosis of the Eker renal tumors. [5] Rapamycin inhibits metastatic tumor growth and angiogenesis in CT-26 xenograft models by reducing the production of VEGF and blockage of VEGF-induced endothelial cell signaling. [6] Rapamycin treatment at 4 mg/kg/day significantly reduces tumor growth of C6 xenografts, and tumor vascular permeability. [7]
Animal Research Animal Models Athymic Nu/Nu mice inoculated subcutaneously with VEGF-A-expressing C6 rat glioma cells
Dosages ~4 mg/kg/day
Administration Injection i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06308445 Not yet recruiting
Familial Adenomatous Polyposis
University Hospital Toulouse
 August 1 2024 Phase 2
NCT06310291 Not yet recruiting
Celiac Disease
Barinthus Biotherapeutics
 April 2024 Early Phase 1
NCT06091332 Not yet recruiting
Cavernous Malformations|Brain Stem Hemorrhage
Huashan Hospital
 December 1 2023 Phase 2
NCT05997056 Recruiting
Neuroendocrine Tumors|NET|Pancreatic Neuroendocrine Tumor|Gastrointestinal Neuroendocrine Tumor|Pulmonary Neuroendocrine Tumor
Aadi Bioscience Inc.
 November 7 2023 Phase 2
NCT06022068 Enrolling by invitation
Alzheimer Disease
Karolinska Institutet|Karolinska University Hospital
 September 1 2023 Phase 1|Phase 2
NCT04989686 Recruiting
Immunosuppression
Children''s Hospital of Philadelphia|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)
 June 8 2023 --

Chemical Information & Solubility

Molecular Weight 914.18 Formula

C51H79NO13
CAS No. 53123-88-9 SDF Download Rapamycin SDF
Smiles CC1CCC2CC(C(=CC=CC=CC(CC(C(=O)C(C(C(=CC(C(=O)CC(OC(=O)C3CCCCN3C(=O)C(=O)C1(O2)O)C(C)CC4CCC(C(C4)OC)O)C)C)O)OC)C)C)C)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (109.38 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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