Manumycin A(Synonyms: 手霉素A)

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Manumycin A (Synonyms: 手霉素A) 纯度: ≥98.0%

Manumycin A 是一种抗生素。Manumycin A 作为一种选择性、竞争性的 farnesyltransferase (FTase) 抑制剂,与 farnesylpyrophosphate (Ki =1.2 μM) 有关,并且作为 Ras 蛋白质的非竞争性抑制剂。Manumycin A 诱导细胞凋亡并发挥抗肿瘤活性。Manumycin A 通过靶向抑制 Ras/Raf/ERK1/2 信号转导,抑制外泌体生物发生 (exosome biogenesis) 及分泌。Manumycin A 也是 nSMase 抑制剂 (EC50=0.25 μM)。

Manumycin A(Synonyms: 手霉素A)

Manumycin A Chemical Structure

CAS No. : 52665-74-4

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生物活性

Manumycin A is an antibiotic. Manumycin A acts as a selective, competitive inhibitor of protein farnesyltransferase (FTase) with respect to farnesylpyrophosphate (Ki =1.2 μM), and as a noncompetitive inhibitor with respect to the Ras protein. Manumycin A induces apoptosis and exerts antitumor activity[1] [2][3]. Manumycin A suppresses exosome biogenesis and secretion via targeted inhibition of Ras/Raf/ERK1/2 signaling[4]. Manumycin A is a nSMase inhibitor (EC50=0.25 μM)[5].

IC50 & Target

Farnesyltransferase, Ras, nSMase inhibitor[1][5]

分子量

550.64

Formula

C31H38N2O7

CAS 号

52665-74-4

中文名称

手霉素A

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献
  • [1]. Hara M, et al. Identification of Ras farnesyltransferase inhibitors by microbial screening. Proc Natl Acad Sci U S A. 1993 Mar 15;90(6):2281-5.

    [2]. Bernier M, et al. Binding of manumycin A inhibits IkappaB kinase beta activity. J Biol Chem. 2006 Feb 3;281(5):2551-61.

    [3]. Kim KH, et al. Manumycin A induces apoptosis in malignant pleural mesothelioma through regulation of Sp1 and activation of the mitochondria-related apoptotic pathway. Oncol Rep. 2016 Jul;36(1):117-24.

    [4]. Datta, A. et al. Manumycin A suppresses exosome biogenesis and secretion via targeted inhibition of Ras/Raf/ERK1/2 signaling and hnRNP H1 in Castration resistant prostate cancer cells. Cancer Let. 408, 73–81 (2017).

    [5]. Zhang H, et al. Advances in the discovery of exosome inhibitors in cancer. J Enzyme Inhib Med Chem. 2020;35(1):1322-1330.

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