CAY10585
货号：
10012682-1mg 基本售价：
154.0 元 规格：
1 mg
产品信息
概述| 货号 | 10012682-1mg |
| 描述 | Hypoxia-inducible factor-1 (HIF-1) is a heterodimeric transcription factor composed of a HIF-1α subunit and HIF-1β subunit. Whereas the HIF-1β subunit is constitutively expressed, the HIF-1α subunit is regulated by cellular oxygen levels and therefore plays an important role in maintaining cellular oxygen homeostasis.1,2 Under normoxic conditions, HIF-1α is selectively hydroxylated on proline residues 402 and 577 and targeted for destruction by the ubiquitin-proteasome system. Under hypoxic conditions, HIF-1α accumulates and dimerizes with HIF-1β to promote the transcription of a number of genes involved in angiogenesis, glycolysis, growth factor signaling, tumor invasion, and metastasis. CAY10585 is a novel small molecule inhibitor of HIF-1α accumulation and gene transcriptional activity.3 In a gene reporter assay using human Hep3B and AGS cell lines, CAY10585 prevented HIF-1 transcriptional activity with IC50 values of 2.6 and 0.7 µM, respectively. It blocks HIF-1α accumulation in Hep3B cells in a concentration and time-dependent manner, with complete inhibition at a concentration of 30 µM within 12 hours. CAY10585 also significantly suppresses transcription of the HIF-1 target genes VEGF and erythropoietin at 10 µM.3 |
| 别名 | Hypoxia-Inducible Factor-1α Inhibitor; |
性能| 供应商 | Cayman |
| 应用文献 |
1.Wang, G.L.,Jiang, B.H.,Rue, E.A., et al. Hypoxia-inducible factor 1 is a basic-helix-loop-helix-PAS heterodimer regulated by cellular O2 tension. Proceedings of the National Academy of Sciences of the United States of America 92, 5510-5514 (1995).
2.Safran, M., and Kaelin, W.G., Jr. HIF hydroxylation and the mammalian oxygen-sensing pathway. Journal of Clinical Investigation 111, 779-783 (2003).
3.Lee, K.,Lee, J.H.,Boovanahalli, S.K., et al. (Aryloxyacetylamino)benzoic acid analogues: A new class of hypoxia-inducible factor-1 inhibitors. Journal of Medicinal Chemistry 50, 1675-1684 (2007).
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| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥97% |
| 计算分子量 | 435.5 |
| 分子式 | C26H29NO5 |
| CAS号 | 934593-90-5 |
| 稳定性 | ≥ 2 years |
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