Rapamycin [53123-88-9]

Catalog number: HY-10219_100mg
Brand: MedChem Express
Packing: 100 mg
Other sizes: Also available in other sizes.
Price: € 108.00
Expected delivery time: 10 days

Product specifications for - Rapamycin [53123-88-9]

Product group: Chemicals
Category: Other
CAS No.: 53123-88-9
Purity: >98%
Molecular Formula: C51H79NO13
Molecular weight: 914.17
Datasheet: Datasheet
  Research Use Only
UNSPSC: 12352200
Scientific information: 
Scientific info: Rapamycin (Sirolimus, AY-22989, WY-090217) is a specific mTOR inhibitor with IC50 of 0.1 nM. IC50 value: 0.1 nM [1] Target: mTOR 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 uM, respectively, while displaying little activity against U373-MG cells with IC50 of >25 uM 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]. 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].
Safety information: 
Effects of molecularly targeted therapies on murine thymus: highly selective mTOR inhibitors induce reversible thymic involution', S Al-Hammadi. Exp Hematol Oncol. 2016 Jul 29;5:22. Read more
Anhydroicaritin improves diet-induced obesity and hyperlipidemia and alleviates insulin resistance by suppressing SREBPs activation', Zheng ZG. Biochem Pharmacol. 2016 Dec 15;122:42-61. Read more
Codon bias imposes a targetable limitation on KRAS-driven therapeutic resistance', Ali M. Nat Commun. 2017 Jun 8;8:15617. Read more
MicroRNA-144-3p inhibits autophagy activation and enhances Bacillus Calmette-Guérin infection by targeting ATG4a in RAW264.7 macrophage cells', Guo L. PLoS One. 2017 Jun 21;12(6):e0179772. Read more
Sirolimus alters lung pathology and viral load following influenza A virus infection', Alsuwaidi AR. Respir Res. 2017 Jul 11;18(1):136. Read more
Activin-A enhances mTOR signaling to promote aberrant chondrogenesis in fibrodysplasia ossificans progressiva', Hino K. J Clin Invest. 2017 Sep 1;127(9):3339-3352. Read more
Krüppel-like factor 6 is a transcriptional activator of autophagy in acute liver injury', Sydor S. Sci Rep. 2017 Aug 14;7(1):8119. Read more
Autophagy mediates free fatty acid effects on MDA‑MB‑231 cell proliferation, migration and invasion', Juan Wu. Oncol Lett. 2017 Oct;14(4):4715-4721. Read more
Fingolimod suppresses neuronal autophagy through the mTOR/p70S6K pathway and alleviates ischemic brain damage in mice', Li X. PLoS One. 2017 Nov 29;12(11):e0188748. Read more
RA and ω-3 PUFA co-treatment activates autophagy in cancer cells', Zhu S. Oncotarget. 2017 Nov 22;8(65):109135-109150. Read more