| 货号 | 14436-1mg |
| 描述 | Borrelidin is a secondary metabolite produced by Streptomyces and other bacteria. It displays potent antiangiogenic activity, preventing tube formation in rat aorta explants (IC50 = 0.8 nM) and inducing apoptosis in endothelial cells.1,2 Borrelidin also alters the splicing of VEGF mRNA, producing an antiangiogenic isoform of the growth factor.3 It has long been known as a powerful inhibitor of both eukaryotic and bacterial threonyl tRNA synthetase.4 Borrelidin is also an effective anti-malarial drug, as it kills P. falciparum with an IC50 value of 1.8 nM.5 At higher doses, it inhibits cyclin-dependent kinase in yeast (IC50 = 24 μM), resulting in growth arrest in the G1phase.6 |
| 别名 | NSC 216128;Treponemycin; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Wakabayashi, T.,Kageyama, R.,Naruse, N., et al. Borrelidin is an angiogenesis inhibitor; Disruption of angiogenic capillary vessels in a rat aorta matrix culture model. Journal of Antibiotics 50(8), 671-676 (1997). 2.Kawamura, T.,Liu, D.,Towle, M.J., et al. Anti-angiogenesis effects of borrelidin are mediated through distinct pathways: Threonyl-tRNA synthetase and caspases are independently involved in suppression of proliferation and induction of apoptosis in endothelial cells. Journal of Antibiotics 56(8), 709-715 (2003). 3.Woolard, J.,Vousden, W.,Moss, S.J., et al. Borrelidin modulates the alternative splicing of VEGF in favour of anti-angiogenic isoforms. Chem.Sci. 2011(2), 273-278 (2011). 4.Paetz, W. and Nass, G. Biochemical and immunological characterization of threonyl-tRNA synthetase of two borrelidin-resistant mutants of Escherichia coli K12. European Journal of Biochemistry 35, 331-337 (1973). 5.Otoguro, K.,Ui, H.,Ishiyama, A., et al. In vitro and in vivo antimalarial activities of a non-glycosidic 18-membered macrolide antibiotic, borrelidin, against drug-resistant strains of Plasmodia. Journal of Antibiotics 56(8), 727-729 (2003). 6.Tsuchiya, E.,Yukawa, M.,Miyakawa, T., et al. Borrelidin inhibits a cyclin-dependent kinase (CDK), Cdc28/Cln2, of Saccharomyces cerevisiae. Journal of Antibiotics 54(1), 84-90 (2001). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 489.6 |
| 分子式 | C28H43NO6 |
| CAS号 | 7184-60-3 |
| 稳定性 | ≥ 1 year |
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