Pironetin

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Pironetin 

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。

Pironetin

Pironetin Chemical Structure

CAS No. : 151519-02-7

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生物活性

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].

IC50 & Target

Microtubule[1]

体外研究
(In Vitro)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

Cell Line: 3Y1 cells
Concentration: 20 ng/mL, 50 ng/mL, 100 ng/mL
Incubation Time: 24 hours
Result: Arrested the cell cycle progression at G2/M in3Y1 cells.

Cell Proliferation Assay[1]

Cell Line: HeLa, A2780 and K-NRK cells
Concentration: 1 ng/mL, 10 ng/mL, 100 ng/mL, 1000 ng/mL and 10000 ng/mL
Incubation Time: 3 days
Result: Inhibited the cell proliferation.

体内研究
(In Vivo)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female CDF1-SLC mice (10 weeks) injected with P388 murine leukemia cells[1]
Dosage: 0.78 mg/kg, 1.56 mg/kg, 3.13 mg/kg, 6.25 mg/kg
Administration: Intraperitoneal injection; daily; for 5 days
Result: Showed a moderate antitumor effect.

分子量

324.45

Formula

C19H32O4

CAS 号

151519-02-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [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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