| 货号 | 16427-1mg |
| 描述 | LAQ824 is a hydroxamate-based inhibitor of histone deacetylases (HDACs) with an IC50 value of 30 nM.1,2 It inhibits the growth of colon, breast, prostate, and non-small cell lung cancer cell lines at concentrations of less than 1 µM.1,3 LAQ824 augments the actions of fludarabine (Item No. 14128) and imatinib mesylate (Item No. 13139) in human leukemia cells.4,5 Through its effects on HDACs, LAQ824 induces acetylation of histones, α-tubulin, and heat shock protein 90 (Hsp90).5,6 Acetylation of Hsp90 blocks its chaperone function, resulting in changes in levels of several client proteins, including estrogen receptor-α, Hsp72, and Raf-1.6,7 |
| 别名 | Dacinostat;NVP-LAQ824; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Catley, L.,Weisberg, E.,Tai, Y.T., et al. NVP-LAQ824 is a potent novel histone deacetylase inhibitor with significant activity against multiple myeloma. Blood 102(7), 2615-2622 (2003). 2.Dokmanovic, M.,Clarke, C. and Marks, P.A. Histone deacetylase inhibitors: Overview and perspectives. Molecular Cancer Research 5(10), 981-989 (2007). 3.Zheng, Y.G.,Wu, J.,Chen, Z., et al. Chemical regulation of epigenetic modifications: Opportunities for new cancer therapy. Medicinal Research Reviews 28(5), 645-687 (2008). 4.Rosato, R.R.,Almenara, J.A.,Maggio, S.C., et al. Role of histone deacetylase inhibitor-induced reactive oxygen species and DNA damage in LAQ-824/fludarabine antileukemic interactions. Molecular Cancer Therapeutics 7(10), 3285-3297 (2008). 5.Nimmanapalli, R.,Fuino, L.,Bali, P., et al. Histone deacetylase inhibitor LAQ824 both lowers expression and promotes proteasomal degradation of Bcr-Abl and induces apoptosis of imatinib mesylate-sensitive or -refractory chronic myelogenous leukemia-blast crisis cells. Cancer Research 63(16), 5126-5135 (2003). 6.Fiskus, W.,Ren, Y.,Mohapatra, A., et al. Hydroxamic acid analogue histone deacetylase inhibitors attenuate estrogen receptor-α levels and transcriptional activity: A result of hyperacetylation and inhibition of chaperone function of heat shock protein 90. Clinical Cancer Research 13(16), 4882-4890 (2007). 7.de Bono, J.S.,Kristeleit, R.,Tolcher, A., et al. Phase I pharmacokinetic and pharmacodynamic study of LAQ824, a hydroxamate histone deacetylase inhibitor with a heat shock protein-90 inhibitory profile, in patients with advanced solid tumors. Clinical Cancer Research 14(20), 6663-6673 (2008). | |
| 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 | 379.5 |
| 分子式 | C22H25N3O3 |
| CAS号 | 404951-53-7 |
| 稳定性 | ≥ 2 years |
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