Rapamycin is a bacterial macrolide with antifungal and immunosuppressant activities (1). Rapamycin forms a complex with the immunophilin FKBP12 which then inhibits the activity of FRAP/mTOR (TOR in yeast) (2,3). Rapamycin treatment of cells leads to the dephosphorylation and inactivation of p70 S6 kinase. Rapamycin also leads to the dephosphorylation of 4E-BP1/PHAS1, thereby promoting its binding to and inactivation of eIF4E (4,5). This activity has been shown to be the basis for Rapamycins ability to block protein synthesis and to arrest cell cycle progression in the G1-phase (6,7). However, it has been suggested that Rapamycins inhibition of the G1/S transition may be the consequence of its effect on cyclin D1 mRNA and protein stability (8). Synonyms: Sirolimus, Rapamune, NSC 226080, Antibiotic AY-22989, WY-090217, RAPA, SILA 9268A, CCRIS 9024, mTOR Inhibitor, 23,27-Epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclohentriacontine CAS No: 53123-88-9 Molecular Formula: C51H79NO13 Molecular Weight: 914.17 Appearance: White to off-white crystalline powder Purity: 99% Melting Point: 173-187C Heavy Metals: 0.002% Moisture: 0.5% Solubility: Soluble in DMSO and methanol. Applications: Suitable for use in in vitro or cell based assays. Other applications not tested. Recommended Dilutions: Dilute into aqueous buffers to yield desired concentrations with final DMSO concentrations of ~0.1%. IC50 values for inhibitory activity against FRAP/mTOR are around 50pM. Such inhibitory activity is seen in cultured cells stimulated with fetal calf serum or a variety of growth factors. For experiments with cultured cells, pretreat with 10nM of R1137-01 for one hour prior to stimulation. Optimal dilutions to be determined by the researcher. Storage and Stability: Powder may be stored at 4C for short-term only. For long-term storage, store at -20C. Stable for 6 months after receipt.
Molecular Weight:
914.17
Purity:
99%
Form:
White to off-white crystalline powder
CAS Number:
[53123-88-9]
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