Rapamycin雷帕霉素

Biological Activity

Rapamycin (also known as Sirolimus and AY-22989), is a highly potent immunosuppressant used primarily to prevent rejection in organ and bone marrow transplant. Rapamycin specifically binds to immunophilin, FK binding protein-12 (FKBP-12) to form a complex that directly binds to FRB domain of mTOR and thus inhibits its activity ^[1-3]. In IL-2-stimulated T cells, Rapamycin impedes cell progression through the G1/S transition of the proliferation cycle,resulting in a mid-to-late G1 arrest via two major mechanism of action, first the Rapamycin-FKBP-mTOR complex blocks the phosphorylation/activation of the 70 kd S6 protein kinases (pp70S6K), an early event of cytokine-induced mitogenic response; A second the complex suppresses the enzymatic activity of the cyclin-dependent kinase cdk2-cyclin E complex, which functions as a crucial regulator of G1/S transition ^[4-5]. Rapamycin shows antitumor properties by halting tumor cell proliferation, inducing tumor cell apoptosis, and suppressing tumor angiogenesis ^[6]. Rapamycin extends median and maximal lifespan of both male and female mice when feed beginning at 600 days of age ^[7]. [Note: Rapamycin sold by Gene Operation is for scientific research use only, not for human and veterinary use.]

Chemical Properties

Cas No.: 53123-88-9	M. Wt.: 914.17
Formula: C51H79NO13	Purity: >99%
Synonym: Sirolimus, AY-22989, RAPA, NSC 226080, Rapamune®
Chemical Name: (3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,10,12,13,14,21,22,23,24,­25, 26,27,32,33,34,34a-Hexadecahydro-9,27-dihydroxy-3-[(1R)-2-[(1S,3R,4R)-4-hydroxy-3-methoxycyclohexyl]- 1-methylethyl]-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-23,27-epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclohentriacontine-1,5,11,28,29(4H,6H,31H)-pentone
Appearance: White to off-white crystalline powder
Solubility: Soluble in DMSO and ethanol at 50 mg/mL. Very poorly soluble in water.
Storage: Store powder at -20 ºC for the stability up to two years.