457070-06-3

Cytostatin is a natural antitumor inhibitor of cell adhesion to extracellular matrix, blocking adhesion of B16 melanoma cells to laminin and collagen type IV in vitro (IC₅₀s = 1.3 and 1.4 μg/ml, respectively) and B16 cells metastatic activity in mice.^1,2 It induces apoptosis of FS3 mouse fibrosarcoma cells (IC₅₀ = 3.1 μg/ml).³ Cytostatin potently and selectively inhibits protein phosphatase 2A (PP2A; IC₅₀ = 29 nM against the catalytic subunit), while having no effect against PP1, PP2B, or PP5.^4,5

Cytostatin sodium is an effective and selective protein phosphatase 2A (PP2A) inhibitor with an IC50 value of 210 nM. Cytostatin sodium exhibits anti-metastatic properties, good antitumor activity, and can induce apoptosis. Cytostatin sodium can also prevent the adhesion of B16 melanoma cells to components of the extracellular matrix (laminin and collagen). Cytostatin sodium belongs to the family of natural product fosriecin[1][2][3][4].

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1. Amemiya, M., Ueno, M., Osono, M., et al. Cytostatin, a novel inhibitor of cell adhesion to components of extracellular matrix produced by Streptomyces sp. MJ654-NF4. I. Taxonomy, fermentation, isolation and biological activities J. Antibiot. (Tokyo) 47(5),536-540(1994).
2. Masuda, T., Watanabe, S.-i., Amemiya, M., et al. Inhibitory effect of cytostatin on spontaneous lung metastases of B16-BL6 melanoma cells J. Antibiot. (Tokyo) 48(6),528-529(1995).
3. Yamazaki, K., Amemiya, M., Ishizuka, M., et al. Screening for apoptosis inducers in microbial products and induction of apoptosis by cytostatin J. Antibiot. (Tokyo) 48(10),1138-1140(1995).
4. Kawada, M., Amemiya, M., Ishizuka, M., et al. Cytostatin, an inhibitor of cell adhesion to extracellular matrix, selectively inhibits protein phosphatase 2A Biochim. Biophys. Acta 1452(2),209-217(1999).
5. Swingle, M.R., Amable, L., Lawhorn, B.G., et al. Structure-activity relationship studies of fostriecin, cytostatin, and key analogs, with PP1, PP2A, PP5, and (β12-β13)-chimeras (PP1/PP2A and PP5/PP2A), provide further insight into the inhibitory actions of fostriecin family inhibitors J. Pharmacol. Exp. Ther. 331(1),45-53(2009).