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Fostriecin (CAS 87860-39-7)

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Alternate Names:
Phosphotrienin; Fostriecin Sodium Salt
Application:
Fostriecin is a Topo II, PP1, and PP2A inhibitor
CAS Number:
87860-39-7
Purity:
≥95%
Molecular Weight:
452.37
Molecular Formula:
C19H26O9P•Na
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Fostriecin is an antibiotic that can be found in Streptomyces pulveraceus. This compound may act to inhibit the catalytic activity of partially purified Topo II (type II topoisomerase) in a non-competitive manner. Unlike other known inhibitors of this enzyme, fosteriecin has not been observed to cause DNA strand breaks in L1210 cells, suggesting that it does not stabilize a cleavable complex. Furthermore, in the same experiment, this agent was demonstrated to cause a block in the G2 phase of the cell cycle. Fostriecin has also displayed a strong capacity to inhibit protein phosphatase 1 (PP1) and protein phosphatase 2A (PP2A).


Fostriecin (CAS 87860-39-7) References

  1. Phase I and pharmacokinetic study of the topoisomerase II catalytic inhibitor fostriecin.  |  de Jong, RS., et al. 1999. Br J Cancer. 79: 882-7. PMID: 10070885
  2. Versatile enantiocontrolled synthesis of (+)-fostriecin.  |  Esumi, T., et al. 2002. Chem Commun (Camb). 3042-3. PMID: 12536807
  3. Catalyst-controlled asymmetric synthesis of fostriecin and 8-epi-fostriecin.  |  Maki, K., et al. 2005. J Am Chem Soc. 127: 17111-7. PMID: 16316259
  4. Antitumor antibiotic fostriecin covalently binds to cysteine-269 residue of protein phosphatase 2A catalytic subunit in mammalian cells.  |  Takeuchi, T., et al. 2009. Bioorg Med Chem. 17: 8113-22. PMID: 19857968
  5. Convergent synthesis of fostriecin via selective alkene couplings and regioselective asymmetric dihydroxylation.  |  Robles, O. and McDonald, FE. 2009. Org Lett. 11: 5498-501. PMID: 19902969
  6. Elucidation of the biosynthetic gene cluster and the post-PKS modification mechanism for fostriecin in Streptomyces pulveraceus.  |  Kong, R., et al. 2013. Chem Biol. 20: 45-54. PMID: 23352138
  7. Synthetic Strategies Employed for the Construction of Fostriecin and Related Natural Products.  |  Trost, BM., et al. 2016. Chem Rev. 116: 15035-15088. PMID: 28027648
  8. Effects of fostriecin on β2-adrenoceptor-driven responses in human mast cells.  |  Bastan, R., et al. 2017. J Immunotoxicol. 14: 60-65. PMID: 28090813
  9. Inhibition of type II topoisomerase by fostriecin.  |  Boritzki, TJ., et al. 1988. Biochem Pharmacol. 37: 4063-8. PMID: 2847752
  10. Total and Formal Syntheses of Fostriecin.  |  Dong, G., et al. 2020. Org Chem Front. 7: 3608-3615. PMID: 33184589
  11. Chromosome condensation induced by fostriecin does not require p34cdc2 kinase activity and histone H1 hyperphosphorylation, but is associated with enhanced histone H2A and H3 phosphorylation.  |  Guo, XW., et al. 1995. EMBO J. 14: 976-85. PMID: 7889943
  12. Antitumor drug fostriecin inhibits the mitotic entry checkpoint and protein phosphatases 1 and 2A.  |  Roberge, M., et al. 1994. Cancer Res. 54: 6115-21. PMID: 7954457
  13. Fostriecin, an antitumor antibiotic with inhibitory activity against serine/threonine protein phosphatases types 1 (PP1) and 2A (PP2A), is highly selective for PP2A.  |  Walsh, AH., et al. 1997. FEBS Lett. 416: 230-4. PMID: 9373158
  14. Renal toxicity of the anticancer drug fostriecin.  |  de Jong, RS., et al. 1998. Cancer Chemother Pharmacol. 42: 160-4. PMID: 9654117
  15. Fostriecin, an inhibitor of protein phosphatase 2A, limits myocardial infarct size even when administered after onset of ischemia.  |  Weinbrenner, C., et al. 1998. Circulation. 98: 899-905. PMID: 9738645

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Fostriecin, 50 µg

sc-202160
50 µg
$265.00