| 货号 | 15725-5mg |
| 描述 | Bufalin is a cardiotonic steroid first isolated from toad venom and used in traditional Asian medicine.1,2 It inhibits the Na+/K+-ATPase transporter (Kds = 42, 45, and 40 nM for the α1, α2, and α3 subunits, respectively).3 Intravenously administered bufalin is cleared rapidly, with a plasma half-life of 25 minutes in dogs and rats.4 Bufalin inhibits steroid receptor coactivator 1 (SRC-1) and SRC-3 at doses as low as 5 nM, promotes the degradation of SRC-3 protein, and inhibits cancer cell growth both in vitroandin vivo.5 It can also impact the action and expression of several other proteins and kinases as well as induce apoptosis in various cancer cells.6,7 |
| 别名 | NSC 89595; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Yoshida, S. and Sakai, T. Effects of bufalin and related cardiotonic steroids in the neuromuscular junction. Japanese Journal of Pharmacology 23(6), 859-869 (1973). 2.Pavlovic, D. The role of cardiotonic steroids in the pathogenesis of cardiomyopathy in chronic kidney disease. Nephron Clin.Pract. 128, (2014). 3.Katz, A.,Lifshitz, Y.,Bab-Dinitz, E., et al. Selectivity of digitalis glycosides for isoforms of human Na,K-ATPase. The Journal of Biological Chemisty 285(25), 19582-19592 (2010). 4.Hamlyn, J.M. Natriuretic hormones, endogenous ouabain, and related sodium transport inhibitors. Front.Endocrinol.(Lausanne) 5, (2015). 5.Wang, Y.,Lonard, D.M.,Yu, Y., et al. Bufalin is a potent small-molecule inhibitor of the steroid receptor coactivators SRC-3 and SRC-1. Cancer Research 74(5), 1506-1517 (2014). 6.Wu, S.H.,Hsiao, Y.T.,Kuo, C.L., et al. Bufalin inhibits NCI-H460 human lung cancer cell metastasis in vitro by inhibiting MAPKs, MMPs, and NF-KB pathways. Am.J.Chin.Med. 43(6), 1247-1264 (2015). 7.Yin, P.H.,Liu, X.,Qiu, Y.Y., et al. Anti-tumor activity and apoptosis-regulation mechanisms of bufalin in various cancers: New hope for cancer patients. Asian Pac.J.Cancer Prev. 13(11), 5339-5343 (2012). | |
| 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 | 386.5 |
| 分子式 | C24H34O4 |
| CAS号 | 465-21-4 |
| 稳定性 | ≥ 2 years |
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