Thiostrepton
Thiostrepton is a thiazole antibiotic that exhibits antibacterial and anticancer properties. Thiostrepton inhibits the proteasome, binding 23s rRNA; it inhibits phosphate release after GTP hydrolysis in the ribosome, preventing tRNA translocation and turnover and inhibiting elongation during protein synthesis. Thiostrepton also inhibits the expression of Forkhead box M1 (FOXM1), an oncogenic transcription factor involved in cell cycle progression and oxidative stress responses. This compound alters the electrophoretic mobility of peroxiredoxin 3 (PRX3), disabling mitochondrial antioxidative activities during oxidative stress.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18976188
| Cas No. |
1393-48-2 |
|---|---|
| Purity |
≥97%, HPLC |
| Formula |
C72H85N19O18S5 |
| Formula Wt. |
1664.89 |
| Melting Point |
246-256°C dec. |
| Solubility |
Practically insoluble in water. Soluble in chloroform, dichloromethane, DMF. DMSO solution (1 %) is unstable – should be freshly prepared. |
| Appearance |
White to off white powder |
Newick K, Cunniff B, Preston K, et al. Peroxiredoxin 3 is a redox-dependent target of thiostrepton in malignant mesothelioma cells. PLoS One. 2012;7(6):e39404. PMID: 22761781
Rodnina MV, Savelsbergh A, Matassova NB, et al. Thiostrepton inhibits the turnover but not the GTPase of elongation factor G on the ribosome. Proc Natl Acad Sci U S A. 1999 Aug 17;96(17):9586-90. PMID: 10449736.
Naaktgeboren N, Roobol K, Gubbens J, et al. The mode of action of thiostrepton in the initiation of protein synthesis. Eur J Biochem. 1976 Nov 1;70(1):39-47. PMID: 795651.
