Pironetin (Synonyms: NK 10958, NL 9C, PA 48153c, (–)-Pironetin) |
| Catalog No.GC38456 |
La pironetine est une lactone insaturée α/β isolée des espèces de Streptomyces. La pironétine se lie À l'α-tubuline et est un puissant inhibiteur de la polymérisation des microtubules, et a un arrêt du cycle cellulaire et une activité antitumorale.
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Cas No.: 151519-02-7
Sample solution is provided at 25 µL, 10mM.
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Pironetin is an α/β unsaturated lactone isolated from Streptomyces species. Pironetin binds to α-tubulin and is a potent inhibitor of microtubule polymerization, and has cell cycle arrest and antitumor activity[1][2].
Pironetin (20-100 ng/mL; 24 hours; 3Y1 cells) treatment arrests the cell cycle progression at G2/M in 3Y1 cells[1].Pironetin (1-10000 ng/mL; 3 days; HeLa, A2780 and K-NRK cells) treatment inhibits the cell proliferation. IC50 values against these cell lines are almost 10 ng/mL[1]. Cell Cycle Analysis[1] Cell Line: 3Y1 cells
Pironetin (0.78-6.25 mg/kg; intraperitoneal injection; daily; for 5 days; female CDF1-SLC mice) treatment shows a moderate antitumor effect, however, a severe weight loss is observed as a side effect[1]. Animal Model: Female CDF1-SLC mice (10 weeks) injected with P388 murine leukemia cells[1]
[1]. Kondoh M, et al. Cell cycle arrest and antitumor activity of pironetin and its derivatives. Cancer Lett. 1998 Apr 10;126(1):29-32. [2]. Yang J, et al. Pironetin reacts covalently with cysteine-316 of α-tubulin to destabilize microtubule. ] Nat Commun. 2016 Jun 30;7:12103.
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