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Rapamycin (Sirolimus)Original antifungal antibiotic

Rapamycin (Sirolimus)

Catalog No. A8167
Size Price Stock Qty
10mM (in 1mL DMSO) $210.00 In stock
Evaluation Sample $28.00 In stock
5mg $50.00 In stock
25mg $150.00 In stock
100mg $400.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Marsh KM, Schipper D, et al. "Metabolic Impact of Rapamycin (Sirolimus) and B-Estradiol Using Mouse Embryonic Fibroblasts as a Model for Lymphangioleiomyomatosis." Lung. 2017 Jun 2. PMID:28577037
2. Zhixia Qiu , Shuihong Zhang , et al. "The role of curcumin in disruption of HIF-1α accumulation to alleviate adipose fibrosis via AMPK-mediated mTOR pathway in high-fat diet fed mice." J Funct Foods. 2017 Mar.
3. Deng, Jiangshan, et al. "Identification of the protective role of DJ-1 in hypoglycemic astrocyte injury using proteomics." Journal of proteome research (2015). PMID:26057206
4. Ranjan, Kishu, and Chandramani Pathak. "Expression of cFLIPL Determines the Basal Interaction of Bcl‐2 with Beclin‐1 and Regulates p53 Dependent Ubiquitination of Beclin‐1 During Autophagic Stress." Journal of cellular biochemistry (2015). PMID:26682748
5. Holubova, Kristina, et al. "Rapamycin blocks the antidepressant effect of ketamine in task-dependent manner." Psychopharmacology (2016): 1-21. PMID:27004790
6. Fu J, Ma S, et al. "Long-term Stress with Hyperglucocorticoidemia-induced Hepatic Steatosis with VLDL Overproduction Is Dependent on both 5-HT2 Receptor and 5-HT Synthesis in Liver." Int J Biol Sci. 2016 Jan 1;12(2):219-34. PMID:26884719
7. Hagg A, Colgan TD, et al. "Using AAV vectors expressing the β2-adrenoceptor or associated Gα proteins to modulate skeletal muscle mass and muscle fibre size." Sci Rep. 2016 Mar 14;6:23042. PMID:26972746
8. "Li X, Guo K, et al. "5-HT 2 receptor mediates high-fat diet-induced hepatic steatosis and very low density lipoprotein overproduction in rats." Obes Res Clin Pract. 2016 Apr 28." PMID:26972746

Quality Control

Chemical structure

Rapamycin (Sirolimus)

Related Biological Data

Rapamycin

Related Biological Data

Rapamycin

Related Biological Data

Rapamycin

Related Biological Data

Rapamycin

Related Biological Data

Rapamycin

Related Biological Data

Rapamycin

Related Biological Data

Rapamycin

Biological Activity

Description Rapamycin (Sirolimus, AY-22989, WY-090217) is a specific inhibitor of mTOR with IC50 of ~0.1 nM.
Targets mTOR          
IC50 ~0.1 nM          

Protocol

Cell experiment[1]:

Cell lines

Hepatocyte growth factor (HGF)-induced lens epithelial cells (LECs)

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

10 ng/ml, 72h

Applications

Using cell proliferation, cell viability and flow cytometric apoptosis assays, we found that rapamycin potently not only suppressed proliferation but also induced the apoptosis of LECs in a dose-dependent manner under HGF administration. Further investigation of the underlying mechanism using siRNA transfection revealed that rapamycin could promote apoptosis of LECs via inhibiting HGF-induced phosphorylation of AKT/mTOR, ERK and JAK2/STAT3 signaling molecules. Moreover, the forced expression of AKT, ERK and STAT3 could induce a significant suppression of apoptosis in these cells after treatment of rapamycin.

Animal experiment[1]:

Animal models

Ndufs4(−/−) mice

Dosage form

8 mg/kg every other day, intraperitoneal injection

Applications

Rapamycin, a specific inhibitor of the mechanistic target of rapamycin (mTOR) signaling pathway, robustly enhances survival and attenuates disease progression in a mouse model of Leigh syndrome. Administration of rapamycin to these mice, which are deficient in the mitochondrial respiratory chain subunit Ndufs4 [NADH dehydrogenase (ubiquinone) Fe-S protein 4], delays onset of neurological symptoms, reduces neuroinflammation, and prevents brain lesions. Although the precise mechanism of rescue remains to be determined, rapamycin induces a metabolic shift toward amino acid catabolism and away from glycolysis, alleviating the buildup of glycolytic intermediates. This therapeutic strategy may prove relevant for a broad range of mitochondrial diseases.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

1. Tian F, Dong L, Zhou Y et al. Rapamycin-Induced Apoptosis in HGF-Stimulated Lens Epithelial Cells by AKT/mTOR, ERK and JAK2/STAT3 Pathways. Int J Mol Sci. 2014 Aug 11;15(8):13833-48.

2. Johnson SC1, Yanos ME, Kayser EB et al. mTOR inhibition alleviates mitochondrial disease in a mouse model of Leigh syndrome. Science. 2013 Dec 20;342(6165):1524-8.

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Chemical Properties

Cas No. 53123-88-9 SDF Download SDF
Synonyms Sirolimus,(-)-Rapamycin, AY-22989, WY-090217, Antibiotic AY22989
Canonical SMILES O[C@H]1[C@H](OC)C[C@H](C[C@@H](C)[C@H](CC([C@H](C)/C=C(C)/[C@H]([C@@H](OC)C([C@@H](C[C@@H](/C=C/C=C/C=C(C)/[C@@H](OC)C[C@@H]2CC[C@@H](C)[C@@](C(C(N3[C@H]4CCCC3)=O)=O)(O)O2)C)C)=O)O)=O)OC4=O)CC1
Formula C51H79NO13 M.Wt 914.18
Solubility >45.7mg/mL in DMSO Storage Desiccate at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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Background

Rapamycin was used as a kind of original antifungal antibiotic, which is produced by Streptomyces hygroscopicus. Now it has been used in the prevention of transplant rejection because of its immunosuppressive effect.  It also exhibits activity against several transplantable tumors and slightly activity to inactive against leukemias. The immunosuppressive effect of Rapamycin is exerted by inhibiting the activation and proliferation of T cells. Rapamycin binds to FK-binding protein 12 (FKBP12) and forms the rapamycin-FKBP12 complex, which regulates an enzyme that plays an important role in the progression of the cell cycle.

References:
1. Sehgal, Suren N. "Rapamune®(RAPA, rapamycin, sirolimus): mechanism of action immunosuppressive effect results from blockade of signal transduction and inhibition of cell cycle progression." Clinical biochemistry 31.5 (1998): 335-340.
2. Sehgal, S. N., H. Baker, and Claude Vézina. "Rapamycin (AY-22,989), a new antifungal antibiotic. II. Fermentation, isolation and characterization." The Journal of antibiotics 28.10 (1975): 727-732.