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Rapamycin

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

Rapamycin (AY 22989) is a natural product of macrolides, an mTOR inhibitor with specificity (HEK293 cells: IC50=0.1 nM). Rapamycin has immunosuppressive activity and induces autophagy.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Rapamycin Chemical Structure
Rapamycin, CAS 53123-88-9
Pack Size Availability Price/USD Quantity
25 mg In stock $ 40.00
50 mg In stock $ 48.00
100 mg In stock $ 64.00
200 mg In stock $ 110.00
500 mg In stock $ 207.00
1 mL * 10 mM (in DMSO) In stock $ 44.00
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Purity: 98.73%
Purity: 98.09%
Purity: 98.03%
Purity: 97.08%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Rapamycin (AY 22989) is a natural product of macrolides, an mTOR inhibitor with specificity (HEK293 cells: IC50=0.1 nM). Rapamycin has immunosuppressive activity and induces autophagy.
Targets&IC50 mTOR:0.1 nM (HEK293 cells)
In vitro METHODS: Normal human renal epithelial cells HRECs were treated with Rapamycin (0.01-1000 nmol/L) for 6 days, and cell growth inhibition was detected using MTT.
RESULTS: Rapamycin dose-dependently inhibited the growth of HRECs, with a 40% reduction in cell viability at a concentration of 10 nmol/L. [1]
METHODS: Human cervical cancer cells HeLa and human prostate cancer cells PC3 were treated with Rapamycin (100 mM) for 0.5-24 h, and the expression levels of target proteins were detected by Immunoprecipitation.
RESULTS: Rapamycin had little effect on the expression levels of mTOR, raptor and rictor. Rapamycin significantly reduced raptor binding to mTOR at 0.5 h and rictor binding to mTOR at 24 h. Long-term treatment of cells with Rapamycin inhibited mTORC2 assembly. [2]
METHODS: Human vascular endothelial cells were treated with Rapamycin (1-100 ng/mL) for 48 h, and cell migration was examined using the Wound-healing method.
RESULTS: Rapamycin dose-dependently inhibited the migration of human vascular endothelial cells. [3]
In vivo METHODS: To study the effect of Rapamycin on life expectancy, Rapamycin (8 mg/kg in DMSO+5% PEG-400+5% Tween-80) was administered intraperitoneally to 20-21 month old C57BL/6J mice once daily for three months.
RESULTS: Three months of Rapamycin treatment was sufficient to increase the life expectancy of middle-aged mice by 60% and improve their healthy lifespan. [4]
METHODS: To determine the appropriate dose of Rapamycin for the treatment of epilepsy, Rapamycin (0.1-3 mg/kg in 4% ethanol + 5% Tween 80 + 5% PEG 400) was injected intraperitoneally into Sprague-Dawley rats once a day for four weeks.
RESULTS: Only 1.0 mg/kg and 3.0 mg/kg Rapamycin inhibited p-S6. Rats treated with 0.1 and 0.3 mg/kg Rapamycin had no significant adverse effects, whereas rats treated with 1.0 and 3.0 mg/kg Rapamycin showed significant reductions in body, spleen, and thymus weights, and exhibited cognitive impairment and anxiety. The Rapamycin dose could not inhibit mTOR in the treatment of epilepsy without causing any side effects, but 1 mg/kg may be the optimal dose to inhibit mTOR in young rats with relatively few side effects. [5]
Kinase Assay HEK293 cells were plated at 2-2.5 × 10^5 cells per well of a 12-well plate and serum-starved for 24 h in DMEM only. Cells were mock-treated or treated with rapamycin (0.05-50 nM), iRap (0.5-500 nM), or AP21967 (0.5-500 nM) for 15 minutes at 37 °C. Serum was added to a final concentration of 20% for 30 minutes at 37 °C. Cells were lysed as described and cell lysates were separated by SDS-PAGE. Resolved proteins were transferred to a PVDF membrane and immunoblotted with a phosphospecific primary antibody against Thr389 of p70 S6 kinase. Data were analyzed using ImageQuant and KaleidaGraph [1].
Cell Research To determine the effects of rapamycin and rapamycin plus LY294002 or UCN-01 on tumor cells, we determined cell viability after the treatments. We used a trypan blue dye exclusion assay as described previously. Tumor cells in exponential growth were harvested and seeded at 5 × 10^3 cells per well (0.1 mL) in 96-well flat-bottomed plates and incubated overnight at 37°C. The cells were then incubated for 72 hours with or without rapamycin or with rapamycin plus LY294002 or UCN-01. After the cells were collected by trypsinization, they were stained with trypan blue, and the viable cells in each well were counted. The viability of the untreated cells (the control) was considered 100%. Survival fractions were calculated from the mean cell viability of the treated cells [3].
Animal Research Animals were randomized to treatment or vehicle groups so that the mean starting body weights of each group were equal. Drug treatment began on the day of surgery or on the first day of reloading after the 14-day suspension. Rapamycin was delivered once daily by intraperitoneal injection at a dose of 1.5 mg/kg, dissolved in 2% carboxymethylcellulose. CsA was delivered once daily by subcutaneous injection at a dose of 15 mg/kg, dissolved in 10% methanol and olive oil. FK506 was delivered once daily via subcutaneous injection at a dose of 3 mg kg?1, dissolved in 10% ethanol, 10% cremophor and saline [4].
Synonyms Sirolimus, AY 22989, NSC-2260804
Molecular Weight 914.17
Formula C51H79NO13
CAS No. 53123-88-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 100mg/mL (109 mM), Sonification is recommended

H2O: Insoluble

DMSO: 100 mg/mL (109 mM), Sonification is recommended

TargetMolReferences and Literature

1. Pallet N, et al. Rapamycin inhibits human renal epithelial cell proliferation: effect on cyclin D3 mRNA expression and stability. Kidney Int. 2005 Jun;67(6):2422-33. 2. Sarbassov DD, et al. Prolonged rapamycin treatment inhibits mTORC2 assembly and Akt/PKB. Mol Cell. 2006 Apr 21;22(2):159-68. 3. Si Y, et al. Concentration-dependent effects of rapamycin on proliferation, migration and apoptosis of endothelial cells in human venous malformation. Exp Ther Med. 2018 Dec;16(6):4595-4601. 4. Bitto A, et al. Transient rapamycin treatment can increase lifespan and healthspan in middle-aged mice. Elife. 2016 Aug 23;5:e16351. 5. Bishu K, et al. Anti-remodeling effects of rapamycin in experimental heart failure: dose response and interaction with angiotensin receptor blockade. PLoS One. 2013 Dec 3;8(12):e81325. 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.

TargetMolCitations

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A breakdown in microglial metabolic reprogramming causes internalization dysfunction of α-synuclein in a mouse model of Parkinson’s disease. Journal of Neuroinflammation. 2022, 19(1): 1-21 17. Gao C, Yan Y, Chen G, et al. Autophagy Activation Represses Pyroptosis through the IL-13 and JAK1/STAT1 Pathways in a Mouse Model of Moderate Traumatic Brain Injury. ACS Chemical Neuroscience. 2020 18. Cao L, Zhao J, Ma L, et al. Lycopene attenuates zearalenone-induced oxidative damage of piglet sertoli cells through the nuclear factor erythroid-2 related factor signaling pathway. Ecotoxicology and Environmental Safety. 2021, 225: 112737. 19. Wang J L, Wang Y, Gao T T, et al. Venlafaxine protects against chronic stress-related behaviors in mice by activating the mTORC1 signaling cascade. Journal of Affective Disorders. 2020, 276: 525-536. 20. Lei Y, Zhang X, Xu Q, et al. Autophagic elimination of ribosomes during spermiogenesis provides energy for flagellar motility. 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This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Microbial Natural Product Library Pyroptosis Compound Library Anti-Metabolism Disease Compound Library Bioactive Compound Library Preclinical Compound Library ReFRAME Related Library

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Keywords

Rapamycin 53123-88-9 Autophagy Metabolism Microbiology/Virology Others PI3K/Akt/mTOR signaling Endogenous Metabolite Antibiotic mTOR Antifungal Sirolimus AY22989 Bacterial FK506-binding protein immunosuppressant mTORC1 AY 22989 Fungal Mammalian target of Rapamycin inhibit AY-22989 Inhibitor NSC-2260804 NSC2260804 HEK293 FKBP12 FKBP NSC 2260804 inhibitor

 

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