Swinholide A, isolated from the marien sponge Theonella swinhoei, is a 44-carbon ring dimeric dilactone macrolide with a 2-fold axis of symmetry. Recent studies have elucidated its unusual structure and shown that it has potent cytotoxic activity. We now report that swinholide A disrupts the actin cytoskeleton of cells grown in culture, sequesters actin dimers in vitro in both polymerizing and non-polymerizing buffers with a binding stoichiometry of one swinholide A molecule per actin dimer, and rapidly severs F-actin in vitro with high cooperativity. These unique properties are sufficient to explain the cytotoxicity of swinholide A. They also suggest that swinholide A might be a model for studies of the mechanism of action of F-actin severing proteins and be therapeutically useful in conditions where filamentous actin contributes to pathologically high viscosities. Applications: Cell permeable dimeric dilactone macrolide Cytotoxic compound Specific actin filament (F-actin) inhibitor. Disrupts the actin cytoskeleton by sequestering actin dimers and rapidly severing actin filaments (F-actin) Depolymerizes actin filaments (F-actin) Antifungal Apoptosis inducer Alterates the actin cytoskeleton of GH4 cells and inhibits insulin-increased prolactin gene transcription Appearance: Supplied as a colorless oil Purity: 97% (HPLC) Molecular Weight: 1389.9 Source: Isolated from marine sponge Theonella swinhoei Solubility: Soluble in ethanol, methanol, DMSO, acetone or ethyl acetate. Storage and Stability: May be stored at 4C for short-term only. Store at -20C Stable for 6 months after receipt at -20C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
Molekulargewicht:
1389.9
Reinheit:
97% (HPLC)
Formulierung:
Supplied as a colorless oil
CAS Nummer:
[95927-67-6]
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