| 货号 | 16919-10mg |
| 描述 | HDACs are a family of proteins with diverse roles. HDAC6 is a class IIb histone that deacetylates cytoplasmic proteins, including tubulin, heat shock protein 90, and cortactin, and has roles in cell adhesion and motility.1 HDAC8, on the other hand, is a class I histone that primarily targets nuclear proteins, including histones and cohesins, and regulates gene expression.2,3 BRD73954 is a small molecule inhibitor that potently inhibits both HDAC6 and HDAC8 (IC50s = 36 and 120 nM, respectively).4 It is at least 75-fold less effective against other HDAC isoforms.4 At 10 µM, BRD73954 treatment results in a robust increase in acetylation of α-tubulin, a known HDAC6 substrate, but not histone H3, a substrate for HDAC1, 2, and 3, in HeLa cells.4 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Yang, P.H.,Zhang, L.,Zhang, Y.J., et al. HDAC6: Physiological function and its selective inhibitors for cancer treatment. Drug Discov.Ther. 7(6), 233-242 (2013). 2.Nakagawa, M.,Oda, Y.,Eguchi, T., et al. Expression profile of class I histone deacetylases in human cancer tissues. Oncology Reports 18, 769-774 (2007). 3.Deardorff, M.A.,Bando, M.,Nakato, R., et al. HDAC8 mutations in Cornelia de Lange syndrome affect the cohesin acetylation cycle. Nature 489, 313-317 (2012). 4.Olson, D.E.,Wagner, F.F.,Kaya, T., et al. Discovery of the first histone deacetylase 6/8 dual inhibitors. Journal of Medicinal Chemistry 26(11), 4816-4820 (2013). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 284.3 |
| 分子式 | C16H16N2O3 |
| CAS号 | 1440209-96-0 |
| 稳定性 | ≥ 2 years |
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