| 货号 | 14604-1mg |
| 描述 | The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferases G9a and G9a-like protein (GLP) can mono- or dimethylate lysine 9 on histone 3, contributing to early embryogenesis, genomic imprinting, and lymphocyte development.1,2,3 UNC0642 is a selective inhibitor of G9a and GLP that competitively inhibits binding of H3K9 substrates with a Ki = 3.7 nM. It exhibits >2,000-fold selectivity over the lysine methyltransferase EZH2 and >20,000-fold selectivity over other methyltransferases.4 UNC0642 has been shown to reduce H3K9 dimethylation levels in MDA-MB-231 and PANC-1 cells with IC50 values of 110 and 40 nM, respectively.4 Furthermore, it displays improved pharmacokinetic properties relative to UNC0638 (Item No. 10734).4 See the Structural Genomics Consortium (SGC) website for more information. |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Tachibana, M.,Sugimoto, K.,Nozaki, M., et al. G9a histone methyltransferase plays a dominant role in euchromatic histone H3 lysine 9 methylation and is essential for early embryogenesis. Genes & Development 16, 1779-1791 (2002). 2.Wagschal, A.,Sutherland, H.G.,Woodfine, K., et al. G9a histone methyltransferase contributes to imprinting in the mouse placenta. Molecular and Cellular Biology 28(3), 1104-1113 (2008). 3.Thomas, L.R.,Miyashita, H.,Cobb, R.M., et al. Functional analysis of histone methyltransferase G9a in B and T lymphocytes. Journal of Immunology 181, 485-493 (2008). 4.Liu, F.,Barsyte-Lovejoy, D.,Li, F., et al. Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP. Journal of Medicinal Chemistry 56(21), 8931-8942 (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 | 546.7 |
| 分子式 | C29H44F2N6O2 |
| CAS号 | 1481677-78-4 |
| 稳定性 | ≥ 2 years |
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