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产品介绍：
中文名: 雷帕霉素;西罗莫司
英文名: Sirolimus;Rapamycin；AY 22989；FRAP；FAFT
Rapamycin也称AY 22989或sirolimus，可与FKBP12形成复合物，随后结合并抑制FRAP/mTOR。mTOR是哺乳动物中rapamycin的作用靶点，也被称为FRAP或FAFT，是一个Ser/Thr蛋白激酶，可以激活p70 S6 kinase。Rapamycin对于p70 S6 kinase的抑制作用的IC50为0.05nM。Rapamycin通过抑制FRAP/mTOR可以抑制p70 S6 kinase的磷酸化和激活，抑制4E-BP1/PHAS1的磷酸化并促进其对eIF4E的结合和抑制。
LC Laboratories相关资料如下:
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). |