Siomycin A
Siomycin A structure
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Common Name | Siomycin A | ||
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| CAS Number | 12656-09-6 | Molecular Weight | 1648.844 | |
| Density | 1.7±0.1 g/cm3 | Boiling Point | N/A | |
| Molecular Formula | C71H81N19O18S5 | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | N/A | |
Use of Siomycin ASiomycin A is a thiopeptide antibiotic and is a Forkhead box M1(FOXM1) selective inhibitor without affecting other members of the Forkhead box family. Siomycin A has anti-tumor and promotes apoptosis[1][2]. |
| Name | Thiostrepton, 1-valine-2-(2,3-didehydroalanine) |
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| Synonym | More Synonyms |
| Description | Siomycin A is a thiopeptide antibiotic and is a Forkhead box M1(FOXM1) selective inhibitor without affecting other members of the Forkhead box family. Siomycin A has anti-tumor and promotes apoptosis[1][2]. |
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| Related Catalog | |
| Target |
Forkhead box M1(FOXM1)[1] |
| In Vitro | 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 IC50 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 IC50 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[1]. Siomycin A (0-10 µM; MiaPaCa-2 cells) treatment has potent proapoptotic effect in MiaPaCa-2 cells[1]. 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[1]. Cell Viability Assay[1] 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[1] 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[1] 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. |
| In Vivo | Siomycin A (1 µM; subcutaneous injection; for 4 weeks; male Balb/c nude mice) pretreatment decreases tumour growth in an in vivo mouse model[2]. Animal Model: Four- to five-week old male Balb/c nude mice with IOMM-LEE cells[2] Dosage: 1 µM-pretreated IOMM-Lee cells Administration: Subcutaneous injection; for 4 weeks Result: Decreased tumour growth in an in vivo mouse model. |
| References |
| Density | 1.7±0.1 g/cm3 |
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| Molecular Formula | C71H81N19O18S5 |
| Molecular Weight | 1648.844 |
| Exact Mass | 1647.461060 |
| PSA | 701.00000 |
| LogP | -8.95 |
| Index of Refraction | 1.773 |
| RIDADR | NONH for all modes of transport |
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A novel mode of FoxM1 regulation: positive auto-regulatory loop.
Cell Cycle 8(12) , 1966-7, (2009) Oncogenic transcription factor FoxM1 represents an attractive therapeutic target in the fight against cancer, because it is overexpressed in a majority of human tumors. Previously, we identified the t... |
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Thiazole antibiotics target FoxM1 and induce apoptosis in human cancer cells.
PLoS ONE 4(5) , e5592, (2009) Forkhead box M1 (FoxM1) oncogenic transcription factor represents an attractive therapeutic target in the fight against cancer, because it is overexpressed in a majority of human tumors. Recently, usi... |
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The maternal embryonic leucine zipper kinase (MELK) is upregulated in high-grade prostate cancer.
J. Mol. Med. 91(2) , 237-48, (2013) Loss of cell cycle control is a prerequisite for cancer onset and progression. In prostate cancer, increased activity of cell cycle genes has been associated with prognostic parameters such as biochem... |
| siomycin A |
| Antibiotic 6741-21,Mutabillicin,Mutabilycin |
| (1-L-valine)-[2-(2,3-didehydro-alanine)]-thiostrepton |
| N-{3-[(3-Amino-3-oxo-1-propen-2-yl)amino]-3-oxo-1-propen-2-yl}-2-[(11Z)-18-(2,3-dihydroxy-2-butanyl)-11-ethylidene-59-hydroxy-8,31-bis(1-hydroxyethyl)-37-isopropyl-26,46-dimethyl-40,43-bis(methylene)- ;6,9,16,23,28,38,41,44,47-nonaoxo-27-oxa-3,13,20,56-tetrathia-7,10,17,24,36,39,42,45,48,52,58,61,62,63,64-pentadecaazanonacyclo[23.23.9.3.1.1.1.1.0.0]tetra hexaconta-2(64),4,12(63),19(62),21,29,31,33, |