英文名: Sirolimus;Rapamycin；AY 22989；FRAP；FAFT
中文名: 雷帕霉素;西羅莫司
Rapamycin也稱AY 22989或sirolimus，可與FKBP12形成復(fù)合物，隨后結(jié)合并抑制FRAP/mTOR。mTOR是哺乳動(dòng)物中rapamycin的作用靶點(diǎn)，也被稱為FRAP或FAFT，是一個(gè)Ser/Thr蛋白激酶，可以激活p70 S6 kinase。Rapamycin對(duì)于p70 S6 kinase的抑制作用的IC50為0.05nM。Rapamycin通過抑制FRAP/mTOR可以抑制p70 S6 kinase的磷酸化和激活，抑制4E-BP1/PHAS1的磷酸化并促進(jìn)其對(duì)eIF4E的結(jié)合和抑制。
LC Laboratories相關(guān)資料如下:
R-5000 Rapamycin, >99%
M.W. 914.17 C51H79NO13 [53123-88-9]
RTECS:  VE6250000 M.I. 12:  8288 M.I. 14:  8114
Storage:  Store at or below -20 ºC. 
Solubility:  Soluble in DMSO or ethanol （up to about 50 mg/mL for either solvent）. 
Disposal:  A
View the MSDS for this product:
• Immunosuppressant, related to FK-506, but without calcineurin inhibitory activity even when complexed to FK-506 binding protein.  Selectively blocks signaling that leads to p70 S6 kinase activation （IC50 = 50 pM）.  Terada, N., et al.  "Failure of rapamycin to block proliferation once resting cells have entered the cell cycle despite inactivation of p70 S6 kinase."  J. Biol. Chem. 268:  12062-12068 （1993）.  Fingar, D.C., et al.  "Dissociation of pp70 ribosomal protein S6 kinase from insulin-stimulated glucose transport in 3T3-L1 adipocytes."  J. Biol. Chem. 268:  3005-3008 （1993）.  Price, D.J., et al.  "Rapamycin-induced inhibition of the 70-kilodalton S6 protein kinase."  Science 257:  973-977 （1992）.  Chung, J., et al.  "Rapamycin-FKBP specifically blocks growth-dependent activation of and signaling by the 70 kd S6 protein kinases."  Cell 69:  1227-1236 （1992）.
保存條件： -20度