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Fostriecin (Phosphotrienin, CI-920, CL-1565A, NSC-339638, PD 110,161, Pyranone phosphate)

Cat no: 044821


Supplier: United States Biological
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Antibiotic. Anticancer compound. Anti-fungal. Catalytic inhibitor of topoisomerase II (IC50 = 40 microM). Potent protein phosphatase 2A (PP2A) (IC50 = 1. 5 nM) and 4 (PP4) (IC50 = 3 nM) inhibitor. Weak protein phosphatase type 1 (PP1) inhibitor (IC50=131microM). No apparent inhibition on PP2B. Mitotic entry checkpoint inhibitor. Mediates cell cycle arrest at G2-M-phase. Ischemia protective. The PP2A binding site is different from that of okadaic acid Storage and Stability: Short-term Storage: +4 degrees C Long-term Storage: -20 degrees C Stable for at least 2 years after receipt when stored at -20 degrees C.
Catalogue number: 044821
Size: 10ug
Purity: >98% (HPLC)
Alternative names: Phosphotrienin, CI-920, CL-1565A, NSC-339638, PD 110,161, Pyranone phosphate
References: Product Reference: Novel antitumor agents CI-920, PD 113,270 and PD 113,271. I. Taxonomy, fermentation and biological properties: J.B. Tunac, et al.; J. Antibiot. (Tokyo) 36, 1595 (1983)? Novel antitumor agents CI-920, PD 113,270 and PD 113,271. II. Isolation and characterization: S.S. Stampwala, et al.; J. Antibiot. (Tokyo) 36, 1601 (1983)? Studies on the biochemical mechanism of the novel antitumor agent, CI- 920: D.W. Fry, et al.; Cancer Chemother. Pharmacol. 13, 171 (1984)? Anticancer activity of the structurally novel antibiotic Cl-920 and its analogues: W.R. Leopold, et al.; Cancer Res. 44, 1928 (1984)? In vitro activity of the novel antitumor antibiotic fostriecin (CI-920) in a human tumor cloning assay: W. Scheithauer, et al.; Eur. J. Cancer Clin. Oncol. 22, 921 (1986) ? Antimycotic effects of the novel antitumor agents fostriecin (CI-920), PD 113,270 and PD 113,271: S.W. Mamber, et al.; J. Antibiot. (Tokyo) 39, 1467 (1986)? Inhibition of type II topoisomerase by fostriecin: T.J. Boritzki, et al.; Biochem. Pharmacol. 37, 4063 (1988)? Cytostatic and cytotoxic effects of fostriecin on human promyelocytic HL-60 and lymphocytic MOLT-4 leukemic cells: M.A. Hotz, et al.; Cancer Res. 52, 1530 (1992)? Changes in nuclear chromatin related to apoptosis or necrosis induced by the DNA topoisomerase II inhibitor fostriecin in MOLT-4 and HL-60 cells are revealed by altered DNA sensitivity to denaturation: M.A. Hotz, et al.; Exp. Cell Res. 201, 184 (1992)? Antitumor drug fostriecin inhibits the mitotic entry checkpoint and protein phosphatases 1 and 2A: M. Roberge, et al.; Cancer Res. 54, 6115 (1994)? Fostriecin: a review of the preclinical data: R.S. de Jong, et al.; Anticancer Drugs 8, 413 (1997)? Fostriecin, an antitumor antibiotic with inhibitory activity against serine/threonine protein phosphatases types 1 (PP1) and 2A (PP2A), is highly selective for PP2A: A.H. Walsh, et al.; FEBS Lett. 416, 230 (1997)? Fostriecin, an inhibitor of protein phosphatase 2A, limits myocardial infarct size even when administered after onset of ischemia: C. Weinbrenner, et al.; Circulation 98, 899 (1998)? Fostriecin-mediated G2-M-phase growth arrest correlates with abnormal centrosome replication, the formation of aberrant mitotic spindles, and the inhibition of serine/threonine protein phosphatase activity: A. Cheng, et al.; Cancer Res. 58, 3611 (1998)? Purification of protein phosphatase 4 catalytic subunit: inhibition by the antitumour drug fostriecin and other tumour suppressors and promoters: C.J. Hastie & P.T. Cohen; FEBS Lett. 431, 357 (1998)? Phase I and pharmacokinetic study of the topoisomerase II catalytic inhibitor fostriecin: R.S. de Jong, et al.; Br. J. Cancer 79, 882 (1999)? The predicted beta12-beta13 loop is important for inhibition of PP2Acalpha by the antitumor drug fostriecin: D.R. Evans & J.A. Simon; FEBS Lett. 498, 110 (2001)? Fostriecin: chemistry and biology: D.S. Lewy, et al.; Curr. Med. Chem. 9, 2005 (2002)? Antitumor antibiotic fostriecin covalently binds to cysteine-269 residue of protein phosphatase 2A catalytic subunit in mammalian cells: T. Takeuchi, et al.; Bioorg. Med. Chem. 17, 8113 (2009)?

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