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Rapamycin (Sirolimus)Original antifungal antibiotic

Rapamycin (Sirolimus)

Catalog No. A8167
Size Price Stock Qty
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. 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
2. 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
3. Holubova, Kristina, et al. "Rapamycin blocks the antidepressant effect of ketamine in task-dependent manner." Psychopharmacology (2016): 1-21. PMID:27004790
4. 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
5. 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

Quality Control

Chemical structure

Rapamycin (Sirolimus)

Related Biological Data

Rapamycin
Rapamycin, the inhibitor of mTOR, has been reported to promote autophagy in normal cells. We test whether Rapamycin increase the effect of autophagy to 3T3 cells in Western blot assay. The 1mM Rapamycin can inhibit the cell survival of 3T3 cells. Due to the death of cell at the high concentration of Rapamycin, it is not fit to test in Western blot assay. The result has been demonstrated that the low concentration of Rapamycin (1μM) significantly inhibited the P62 and increased the level of autophagy in 3T3 cells.
Method:Western blot; Cell Lines:3T3 cell line; Concentrations:1μM~1mM; Incubation Time:24 h.

Related Biological Data

Rapamycin
Viability of fSMCs was measured with CCK8 assay;the blue line shows viability of cells at the indicated time(24-168 hours) of rapamycin treatment,the red line shows viability of cells at 168 hours and each point indicates the total time in rapamycin,for example,the 24-hour point on the red line shows viability of cells treated for 24 hours with rapamycin followed by 144 hours of rescue in fresh medium(old mdeium was replaced with fresh medium containing or not containing rapamycin every day).

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.

Reacting condition

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

Application

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 Soluble in DMSO > 10 mM 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.