Pironetin 是从链霉菌属物种分离的 α/β 不饱和内酯。Pironetin 与 α-tubulin 结合，是微管聚合的有效抑制剂，具有细胞周期停滞和抗肿瘤活性。
货号:ajcx14804
CAS:151519-02-7
分子式:C19H32O4
分子量：324.45
溶解度:Dichloromethane: soluble,DMSO: soluble,Ethanol: soluble
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.