货号 | 10582-50mg |
描述 | The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development.1,2,3 UNC0321 is a potent and selective G9a HMTase inhibitor, exhibiting a Ki value of 63 pM.4 UNC0321 inhibits G9a with assay-dependent IC50 values of 6-9 nM and GLP, a closely-related H3K9 HMTase, with assay-dependent IC50 values of 15-23 nM.4 It is more than 40,000-fold selective against SET7/9 (a H3K4 HMTase), SET8 (a H4K20 HMTase), PRMT3, and JMJD2E.4 |
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.,Chen, X.,Allali-Hassani, A., et al. Protein lysine methyltransferase G9a inhibitors: Design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines. Journal of Medicinal Chemistry (2010). | |
运输条件 | Wet ice in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥95% |
计算分子量 | 857.8 |
分子式 | C27H45N7O3 • 3(CF3COOH) |
稳定性 | ≥ 1 year |
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