FSL0358
- Structure
- InChI=1S/C14H19NO4/c1-9(16)19-14-12(15-8-13(14)17)7-10-3-5-11(18-2)6-4-10/h3-6,12-15,17H,7-8H2,1-2H3/t12-,13+,14+/m1/s1
- InChIKey=YKJYKKNCCRKFSL-RDBSUJKOSA-N
- Synonyms
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- 22862-76-6
- Ahygroscopin-A
- Anisomycin
- Flagecidin
- NSC-76712
- PA-106
- SA-3097
- Origin
- Streptomyces sp.
- Biological activities
- Inhibition of protein synthesis
- Therapeutic
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Antifungal
- Target
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60S ribosomal subunit
- Assay information
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Inhibition of protein synthesis in vitro using yeast ribosome by binding to 60S ribosomal subunits and blocking peptide bond formation (IC50 = 1 μM)
Preventing elongation of peptide and causing polysome stabilization
Activation of the stress kinases SAPK/JNK and p38 MAPK, as well as p70/85 S6 kinase in mammalian cells, which results in the rapid induction of immediate-early (IE) genes, such as c-fos, fosB, c-jun, JunB, and JunD at a dose of 25 ng/mL, le
Potent signaling agonist, synergizing with growth factors and phorbol esters to superinduce these IE genes
Induction of apoptosis in many cancer cell lines U937 (1 μg/mL) and PC12 cells (10 ng/mL)
- References
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Hazzalin CA, Le Panse R, Cano E, Mahadevan LC
Anisomycin selectively desensitizes signalling components involved in stress kinase activation and fos and jun induction.
Mol Cell Biol, 18(4): 1844-1854 (1998) 9528756
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Kardalinou E, Zhelev N, Hazzalin CA, Mahadevan LC
Anisomycin and rapamycin define an area upstream of p70/85S6k containing a bifurcation to histone H3-HMG-like protein phosphorylation and c-fos-c-jun induction.
Mol Cell Biol, 14(2): 1066-1074 (1994) 8289787
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Kochi SK, Collier RJ
DNA fragmentation and cytolysis in U937 cells treated with diphtheria toxin or other inhibitors of protein synthesis.
Exp Cell Res, 208(1): 296-302 (1993) 8359223 doi: 10.1006/excr.1993.1249
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Barbacid M, Vazquez D
(3H)anisomycin binding to eukaryotic ribosomes.
J Mol Biol, 84(4): 603-623 (1974) 4601392
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Barbacid M, Vazquez D
Preparation of pure (3H)anisomycin by tritium exchange labeling.
Anal Biochem, 56(1): 16-25 (1973) 4764685
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Battaner E, Vazquez D
Inhibitors of protein synthesis by ribosomes of the 80-S type.
Biochim Biophys Acta, 254(2): 316-330 (1971) 4944566
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J. Am. Chem. Soc., 76: 4053 (1954)