盐屋霉素A
- CAS号:12656-09-6
- 英文名:siomycin A
- 中文名:盐屋霉素A
- CBNumber:CB91371285
- 分子式:C71H81N19O18S5
- 分子量:1648.84
- MOL File:12656-09-6.mol
- 密度 :1.65±0.1 g/cm3(Predicted)
- 储存条件 :-20°C
- 溶解度 :DMSO: complete10 mg/ml, clear, colorless to faintly yellow
- 形态 :White solid.
- 酸度系数(pKa) :10.43±0.46(Predicted)
- WGK Germany :3
盐屋霉素A性质、用途与生产工艺
- 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)
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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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