| 货号 | 13631-50mg |
| 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 UNC0224 is a potent and selective G9a HMTase inhibitor, exhibiting an IC50 value of 15 nM.4 Isothermal titration calorimetry revealed UNC0224 binds to G9a with a Kd value of 29 nM. UNC0224 also inhibits GLP, a closely-related H3K9 HMTase, with assay-dependent IC50 values of 20-58 nM, but is more than 1,000-fold selective against SET7/9 (a H3K4 HMTase) and SET8 (a H4K20 HMTase).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. Discovery of a 2,4-diamino-7-aminoalkoxyquinazoline as a potent and selective inhibitor of histone lysine methyltransferase G9a. Journal of Medicinal Chemistry (2009). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 485.7 |
| 分子式 | C26H43N7O2 |
| CAS号 | 1197196-48-7 |
| 稳定性 | ≥ 2 years |
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