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12656-09-6

中文名称 盐屋霉素A
CAS 12656-09-6
分子式 C71H81N19O18S5
分子量 1648.84
MOL 文件 12656-09-6.mol
12656-09-6 结构式 12656-09-6 结构式

基本信息

中文别名
盐霉素 A
盐屋霉素A
英文别名
siomycin A
Mutabilycin
Mutabillicin
Antibiotic 6741-21
AKFVOKPQHFBYCA-OFENGFFDSA-N
Mutabilycin, SporangioMycin, 6741-21, Mutabillicin
Alaninamide, N-[(7R,8S)-2-carboxy-7,8-dihydro-8-hydroxy-4-[(1S)-1-hydroxyethyl]-7-quinolinyl]-L-valyl-2,3-didehydroalanyl-2,3-didehydroalanyl-L-alanyl-2-[(4aR,11S,14Z,18S,21S,28S,32aS)-4a-amino-21-[(1S,2R)-1,2-dihydroxy-1-methylpropyl]-14-ethylidene-3,4,4a,9,10,11,12,13,14,18,19,20,21,27,28,32a-hexa...

物理化学性质

密度1.65±0.1 g/cm3(Predicted)
储存条件-20°C
溶解度完全溶于DMSO,溶解度为10mg/ml,透明,无色至淡黄色
酸度系数(pKa)10.43±0.46(Predicted)
形态白色固体。

安全数据

WGK Germany3

常见问题列表

生物活性
Siomycin A 是一种硫肽抗生素,也是一种 Forkhead box M1(FOXM1) 选择性抑制剂,而且不影响 Forkhead box 家族其他成员。Siomycin A 具有抗肿瘤作用并促进细胞凋亡。
靶点

Forkhead box M1(FOXM1)

体外研究

Siomycin A (0-10 µM; 24-72 hours; K562, MCF7 and MiaPaCa-2 cells) treatment markedly reduces cell viability in a dose-dependent and a time-dependent association in K562, MCF7 and MiaPaCa-2 cells. Among the three cell lines, the IC 50 of the human leukemia K562 cells is the lowest at 6.25 µM at 24 h, while that for the human pancreatic cancer MiaPaCa-2 cells is 6.38 µM. However, the IC 50 of the human pancreatic cancer MiaPaCa-2 cells at 48 and 72 h are the lowest of the three cell lines, which are 0.76 and 0.54 µM, respectively.
Siomycin A (0-10 µM; MiaPaCa-2 cells) treatment has potent proapoptotic effect in MiaPaCa-2 cells.
Siomycin A (0-10 µM; 24 hours; MiaPaCa-2 cells) treatment significantly reduces the expression levels of MMP-2, MMP-9 and α-tubulin protein in the MiaPaCa-2 cells.

Cell Viability Assay

Cell Line: K562, MCF7 and MiaPaCa-2 cells
Concentration: 0 µM, 0.625 µM, 1.25 µM, 2.5 µM, 5 µM or 10 µM
Incubation Time: 24, 48 and 72 hours
Result: Cell viability was markedly reduced in a dose-dependent and a time-dependent association.

Apoptosis Analysis

Cell Line: MiaPaCa-2 cells
Concentration: 0 µM, 0.625 µM, 1.25 µM, 2.5 µM, 5 µM or 10 µM
Incubation Time:
Result: Promoted apoptosis of MiaPaCa-2 cells.

Western Blot Analysis

Cell Line: MiaPaCa-2 cells
Concentration: 0 µM, 0.625 µM, 1.25 µM, 2.5 µM, 5 µM or 10 µM
Incubation Time: 24 hours
Result: The expression levels of MMP-2 and MMP-9 protein in the MiaPaCa-2 cells were significantly reduced in the 2.5, 5 and 10 µM groups.
体内研究

Siomycin A (1 µM; subcutaneous injection; for 4 weeks; male Balb/c nude mice) pretreatment decreases tumour growth in an in vivo mouse model.

Animal Model: Four- to five-week old male Balb/c nude mice with IOMM-LEE cells
Dosage: 1 µM-pretreated IOMM-Lee cells
Administration: Subcutaneous injection; for 4 weeks
Result: Decreased tumour growth in an in vivo mouse model.
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