| 货号 | 13355-1mg |
| 描述 | Geldanamycin is a benzoquinone ansamycin antibiotic which binds heat shock protein 90 (Hsp90) and its paralog GRP94, altering their actions.1,2,3 Through its interaction with these chaperones, geldanamycin indirectly affects numerous client proteins with roles in diverse cellular processes, including gene expression, cell proliferation, apoptosis, and angiogenesis. For example, geldanamycin inhibits c-jun expression in human colon adenocarcinoma HT29 cells (IC50 = 75 nM), inhibiting AP-1 binding.4 It also reduces signaling through mitogenic signaling proteins and interferes with steroid receptor function.1,5,6,7 Inhibitors of Hsp90, including geldanamycin, show promise in cancer therapy.8 |
| 别名 | NSC 122750; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Whitesell, L.,Mimnaugh, E.G.,De Costa, B., et al. Inhibition of heat shock protein Hsp90-pp60v-src heteroprotein complex formation by benzoquinone ansamycins: Essential role for stress proteins in oncogenic transformation. Proceedings of the National Academy of Sciences of the United States of America 91, 8324-8328 (1994). 2.Hadden, M.K.,Lubbers, D.J., and Blagg, B.S.J. Geldanamycin, radicicol, and chimeric inhibitors of the Hsp90 N-terminal ATP binding site. Current Topics in Medicinal Chemistry 6, 1173-1182 (2006). 3.Chavany, C.,Mimnaugh, E.,Miller, P., et al. p185erbB2 binds to GRP94 in vivo. Dissociation of the p185erbB2/GRP94 heterocomplex by benzoquinone ansamycins precedes depletion of p185erbB2. The Journal of Biological Chemisty 271(9), 4974-4977 (1996). 4.Vasilevskaya, I.A., and ODwyer, P.J. Effects of geldanamycin on signaling through activator-protein 1 in hypoxic HT29 human colon adenocarcinoma cells. Cancer Research 59, 3935-3940 (1999). 5.Stancato, L.F.,Silverstein, A.M.,Owens-Grillo, J.K., et al. The hsp90-binding antibiotic geldanamycin decreases Raf levels and epidermal growth factor signaling without disrupting formation of signaling complexes or reducing the specific enzymatic activity of Raf kinase. The Journal of Biological Chemisty 272(7), 4013-4020 (1997). 6.Fukuyo, Y.,Hunt, C.R., and Horikoshi, N. Geldanamycin and its anti-cancer activities. Cancer Letters 290, 24-35 (2010). 7.Smith, D.F.,Whitesell, L.,Nair, S.C., et al. Progesterone receptor structure and function altered by geldanamycin, an hsp90-binding agent. Molecular and Cellular Biology 15(12), 6804-6812 (1995). 8.Taldone, T.,Sun, W., and Chiosis, G. Discovery and development of heat shock protein 90 inhibitors. Bioorganic & Medicinal Chemistry 17(6), 2225-2235 (2009). | |
| 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 | 560.6 |
| 分子式 | C29H40N2O9 |
| CAS号 | 30562-34-6 |
| 稳定性 | ≥ 2 years |
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