kinases protein kinase inhibitors signaling activators kinase substrates antibodies bioluminescence assays
Rapamycin, 5 mg  

Rapamycin, 5 mg

Synonyms: Sirolimus, Rapamune, AY-22989, RAPA, NSC-226080

potently inhibits downstream signaling from mTOR

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Availability: on stock

160,00 €

Background: Rapamycin potently inhibits downstream signaling from the mammalian target of rapamycin (mTOR) proteins which functions in a signaling pathway to promote tumor growth. These evolutionarily conserved protein kinases coordinate the balance between protein synthesis and protein degradation in response to nutrient quality and quantity. Rapamycin binds to the FK-506 binding protein (FKBP12, Kd = 0.2 nM) and the rapamycin/FKBP12 complex then binds to mTOR and prevents interaction of mTOR with target proteins in this signaling pathway. Rapamycin selectively inhibits the phosphorylation and activation of p70 S6 kinase (p70S6K, IC50 = 50 pM). It prevents the translational activation of IGF-II and inhibits later signaling events such as p110Rb phosphorylation, p34cdk1 kinase activation, and cyclin A synthesis.

Chemical formula: C51H79NO13
Molecular weight: 914.2  g/mol
Purity: >99% (HPLC)
Appearance: White to off-white solid
Solubility: soluble in DMSO and methanol
Appearance: White to off-white solid
Handling: Hygroscopic. Protect from Light and Moisture
CAS number: 53123-88-9

PLEASE NOTE: This product is designed for research purposes and can only be delivered to academic and business customers. 

Product specific literature references:

Chung J, Kuo CJ, Crabtree GR, Blenis J (1992) "Rapamycin-FKBP specifically blocks growth-dependent activation of and signaling by the 70 kd S6 protein kinases" Cell 69(7):1227-36

Kuo CJ, Chung J, Fiorentino DF, Flanagan WM, Blenis J, Crabtree GR (1992) "Rapamycin selectively inhibits interleukin-2 activation of p70 S6 kinase" Nature 358(6381):70-3

Brown EJ, Albers MW, Shin TB, Ichikawa K, Keith CT, Lane WS, Schreiber SL (1994) "A mammalian protein targeted by G1-arresting rapamycin-receptor complex" Nature 369(6483):756-8

Sabatini DM, Erdjument-Bromage H, Lui M, Tempst P, Snyder SH (1994) "RAFT1: a mammalian protein that binds to FKBP12 in a rapamycin-dependent fashion and is homologous to yeast TORs" Cell 78(1):35-43

Nourse J, Firpo E, Flanagan WM, Coats S, Polyak K, Lee MH, Massague J, Crabtree GR, Roberts JM (1994) "Interleukin-2-mediated elimination of the p27Kip1 cyclin-dependent kinase inhibitor prevented by rapamycin" Nature 372(6506):570-3

Choi J, Chen J, Schreiber SL, Clardy J (1996) "Structure of the FKBP12-rapamycin complex interacting with the binding domain of human FRAP" Science 273(5272):239-42

Jefferies HB, Fumagalli S, Dennis PB, Reinhard C, Pearson RB, Thomas G (1997) "Rapamycin suppresses 5\'TOP mRNA translation through inhibition of p70s6k" EMBO J. 16(12):3693-704

Nave BT, Ouwens M, Withers DJ, Alessi DR, Shepherd PR (1999) "Mammalian target of rapamycin is a direct target for protein kinase B: identification of a convergence point for opposing effects of insulin and amino-acid deficiency on protein translation" Biochem. J. 344 Pt 2:427-31

Weisman R, Finkelstein S, Choder M (2001) "Rapamycin blocks sexual development in fission yeast through inhibition of the cellular function of an FKBP12 homolog" J. Biol. Chem. 276(27):24736-42

Raught B, Gingras AC, Sonenberg N (2001) "The target of rapamycin (TOR) proteins" Proc. Natl. Acad. Sci. USA 98(13):7037-44

Peer - Reviewed Citations

Uzcátegui NL1, Carmona-Gutiérrez D, Denninger V, Schoenfeld C, Lang F, Figarella K, Duszenko M. (2007) "Antiproliferative effect of dihydroxyacetone on Trypanosoma brucei bloodstream forms: cell cycle progression, subcellular alterations, and cell death."Antimicrob Agents Chemother.(11):3960-8.