Fostriecin A Topo II, PP1, and PP2A inhibitor

Fostriecin (CAS 87860-39-7)

Fostriecin | CAS 87860-39-7 is rated 5.0 out of 5 by 1.
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Synonym: Phosphotrienin; Fostriecin Sodium Salt
Application: A Topo II, PP1, and PP2A inhibitor
CAS Number: 87860-39-7
Purity: ≥95%
Molecular Weight: 452.37
Molecular Formula: C19H26O9P•Na
* Refer to Certificate of Analysis for lot specific data (including water content).
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Fostriecin is an antibiotic originally derived from Streptomyces pulveraceus. This compound has been shown 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).


References

1. Boritzki, T.J., et al. 1988. Biochem. Pharmacol. 37: 4063-4068. PMID: 2847752
2. Roberge, M., et al. 1994. Cancer Res. 54: 6115-6121. PMID: 7954457
3. Guo, X.W., et al. 1995. EMBO J. 14: 976-985. PMID: 7889943
4. Walsh, A.H., et al. 1997. FEBS Lett. 416: 230-234. PMID: 9373158

Appearance :
Powder
Physical State :
Solid
Derived From :
Streptomyces sp.
Solubility :
Soluble in water (100 mM), and methanol. optimal stability in aqueous buffered solutions at pH 6.5. NB: hydrolysis of the phosphate ester will result from inappropriate storage.
Storage :
Store at -20° C
Boiling Point :
737.9° C at 760 mmHg (Predicted)
IC50 :
PP2A: IC50 = 1.5 nM; PP4: IC50 = 3 nM; topoisomerase II: IC50 = 40 µM; PP1: IC50 = 131 µM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
RTECS :
UQ0600000
PubChem CID :
16759606
MDL Number :
MFCD01939908
SMILES :
C[C@](C=C[C@H]1CC=CC(=O)O1)([C@@H](C[C@H](C=CC=CC=CCO)O)O[P](=O)(O)[O-])O.[Na+]

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Certificate of Analysis

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Fostriecin  Product Citations

See how others have used Fostriecin. Click on the entry to view the PubMed entry .

Citations 1 to 6 of 6 total

PMID: # 26196943  Lucas, SJ. et al. 2015. Neuropharmacology. 99: 232-41.

PMID: # 24618897  Williams, BC. et al. 2014. Elife. 3: e01695.

PMID: # 24462681  Amsailale, R. et al. 2014. FEBS Lett. 588: 727-32.

PMID: # 24825897  Kang, Q. et al. 2014. The Journal of biological chemistry. 289: 17480-96.

PMID: # 23536185  Li, Y. et al. 2013. J. Biol. Chem. 288: 13215-24.

PMID: # 22142222  Zgheib, C. et al. 2012. J. Interferon Cytokine Res. 32: 87-94.

Citations 1 to 6 of 6 total
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Rated 5 out of 5 by from Kovacs Kovacs, L. et al. (PubMed 26248159) found that dephosphorylation of calpain-2 at Ser369 was blocked by the protein phosphatase 2A (PP2A) inhibitor fostriecin. -SCBT Publication Review
Date published: 2015-02-10
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