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PI3K/Akt/mTOR signaling mTOR Rapamycin

Rapamycin

Catalog No. T1537   CAS 53123-88-9
Synonyms: AY 22989, Sirolimus, NSC-2260804

Rapamycin, a macrolide compound obtained from Streptomyces hygroscopicus, is a potent and specific mTOR inhibitor (IC50: 0.1 nM in HEK293 cells).

Rapamycin, CAS 53123-88-9
Pack Size Availability Price/USD Quantity
25 mg In stock 40.00
50 mg In stock 59.00
100 mg In stock 75.00
200 mg In stock 123.00
500 mg In stock 231.00
1 mL * 10 mM (in DMSO) In stock 54.00
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Biological Description
Chemical Properties
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Description Rapamycin, a macrolide compound obtained from Streptomyces hygroscopicus, is a potent and specific mTOR inhibitor (IC50: 0.1 nM in HEK293 cells).
Targets&IC50 mTOR : ic50 ~0.1nM,  
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
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. (Only for Reference)
Cell lines: U87-MG, T98G, and U373-MG
Animal Research
Animal Model: Athymic Nu/Nu mice inoculated subcutaneously with VEGF-A-expressing C6 rat glioma cells
Synonyms AY 22989 , Sirolimus , NSC-2260804
Purity 97.08%
Molecular Weight 914.18
Formula C51H79NO13
CAS No. 53123-88-9

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 45.7 mg/mL (50 mM)

Ethanol: 18.3 mg/mL (20 mM)

Water: Insoluble

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

0.5% CMC+0.25% Tween 80: 30 mg/mL

Citations

References and Literature
1. Edwards SR, et al. The rapamycin-binding domain of the protein kinase mammalian target of rapamycin is a destabilizing domain. J Biol Chem. 2007 May 4;282(18):13395-401. 2. Guba M, et al. Rapamycin inhibits primary and metastatic tumor growth by antiangiogenesis: involvement of vascular endothelial growth factor. Nat Med. 2002 Feb;8(2):128-35. 3. Takeuchi H, et al. Synergistic augmentation of rapamycin-induced autophagy in malignant glioma cells by phosphatidylinositol 3-kinase/protein kinase B inhibitors. Cancer Res. 2005 Apr 15;65(8):3336-46. 4. Bodine SC, et al. Akt/mTOR pathway is a crucial regulator of skeletal muscle hypertrophy and can prevent muscle atrophy in vivo. Nat Cell Biol. 2001 Nov;3(11):1014-9. 5. Marin TM, et al. Rapamycin reverses hypertrophic cardiomyopathy in a mouse model of LEOPARD syndrome-associated PTPN11 mutation. J Clin Invest. 2011 Mar;121(3):1026-43. 6. Zhang JW, et al. Metformin synergizes with rapamycin to inhibit the growth of pancreatic cancer in vitro and in vivo. Oncol Lett. 2018 Feb;15(2):1811-1816. 7. Gao C, Wang H, Wang T, et al. Platelet CLEC‐2 regulates neuroinflammation and restores blood brain barrier integrity in a mouse model of traumatic brain injury[J]. Journal of Neurochemistry. 2020: e14983. 8. Zhang T, Tian C, Wu J, et al. . MicroRNA‐182 exacerbates blood‐brain barrier (BBB) disruption by downregulating the mTOR/FOXO1 pathway in cerebral ischemia[J].  The FASEB Journal. 2020, 34(10): 13762-13775. 9. Shang Z, Zhang T, Jiang M, et al. High-carbohydrate, High-fat Diet-induced Hyperlipidemia Hampers the Differentiation Balance of Bone Marrow Mesenchymal Stem Cells by Suppressing Autophagy via the AMPK/mTOR Pathway in Rat Models[J]. 2020. 10. Zhao, Ming, et al. GCG inhibits SARS-CoV-2 replication by disrupting the liquid phase condensation of its nucleocapsid protein. Nature Communications . 12.1 (2021): 1-14.

Related compound libraries

This product is contained In the following compound libraries:
Approved Drug Library Bioactive Compound Library Inhibitor Library Natural Compound Library for HTS Anti-cancer Compound Library Stem cell Differentiation Compound Library Autophagy Compound Library Neuronal Signaling Compound Library Epigenetics Compound Library PI3K-AKT-mTOR Compound Library Tyrosine kinase inhibitor library FDA-approved Drug Library Cytokine Inhibitor Library Kinase Inhibitor Library Bioactive Lipid Compound Library Anti-cancer Approved drug Library Anti-Cardiovascular Disease Compound Library Killers Collection

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