FSL0578
- Structure
- InChI=1S/C20H40N4O10/c1-6(25)14-11(27)10(26)9(23)18(32-14)33-15-7(21)4-8(22)16(12(15)28)34-19-13(29)17(24-3)20(2,30)5-31-19/h6-19,24-30H,4-5,21-23H2,1-3H3/t6-,7+,8-,9-,10-,11+,12+,13-,14-,15-,16+,17-,18-,19-,20+/m1/s1
- InChIKey=BRZYSWJRSDMWLG-DJWUNRQOSA-N
- Synonyms
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- Origin
- Micromonospora echinospora
- Biological activities
- Inhibition of protein synthesis
- Therapeutic
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Antibacterial
Antiprotozoal
Coccidiostats
- Target
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80S ribosomes
- Assay information
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Effective inhibition of wheat-germ, cell-free translation programmed with rat-liver polydenylated RNA (Leading to aberrant protein synthesis in both prokaryotic and eukaryotic cells (IC50 of translation inhibition for Eukaryotic system = 2.0 μM ± 0.3 μM, for Prokaryotic system = 8.9 ± 1.5 nM)
Exhibition of antibacterial activity against B. subtilis (MIC Toxicity for HEK-293, human embryonic kidney cell, LC50 = 1.3 ± 0.1 mM
Inhibition of leishmania promastigotes in the low micromolar range: L. major (LC50 = 1.95 ± 0.05 μM), L. donovani (LC50 = 5.8 ± 0.9 μM)
Fungal growth inhibition of Fusarium graminearum and F. culmorum (MIC = 25 μg/mL in PDA for each, 10 days)
- References
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Yörük E, Albayrak G
Geneticin (G418) resistance and electroporation-mediated transformation of Fusarium graminearum and F. culmorum.
Biotechnol Biotechnol Equip, 29(2): 268-273 (2015) 26019640 doi: 10.1080/13102818.2014.996978
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Lai Y, Diao J, Liu Y, Ishitsuka Y, Su Z, Schulten K, Ha T, Shin YK
Fusion pore formation and expansion induced by Ca2+ and synaptotagmin 1.
Proc Natl Acad Sci U S A, 110(4): 1333-1338 (2013) 23300284 doi: 10.1073/pnas.1218818110
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Nudelman I, Glikin D, Smolkin B, Hainrichson M, Belakhov V, Baasov T
Repairing faulty genes by aminoglycosides: development of new derivatives of geneticin (G418) with enhanced suppression of diseases-causing nonsense mutations.
Bioorg Med Chem, 18(11): 3735-3746 (2010) 20409719 doi: 10.1016/j.bmc.2010.03.060
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Bar-Nun S, Shneyour Y, Beckmann JS
G-418, an elongation inhibitor of 80 S ribosomes.
Biochim Biophys Acta, 741(1): 123-127 (1983) 6193810
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Marvin J. Weinstein, Gerald H. Wagman, Raymond T. Testa, Joseph A. Marquez
(1976). Antibiotic G-418 and the production thereof . US3997403 A.
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Wagman GH, Testa RT, Marquez JA, Weinstein MJ
Antibiotic G-418, a new Micromonospora-produced aminoglycoside with activity against protozoa and helminths: fermentation, isolation, and preliminary characterization.
Antimicrob Agents Chemother, 6(2): 144-149 (1974) 15828184