| 货号 | 10734-50mg |
| 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 UNC0638 is a potent G9a HMTase inhibitor, exhibiting an IC50 value of <15 nM in vitro. UNC0638 also inhibits GLP, a closely-related H3K9 HMTase, with an IC50 value of 19 nM, but is more than 10,000-fold selective against SET7/9 (a H3K4 HMTase), SET8 (a H4K20 HMTase), PRMT3, and SUV39H2. UNC0638 inhibits H3K9 dimethylation in MDA-MB231 cells with an IC50 value of 81 nM and demonstrates favorable separation of functional and toxic effects.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.unlisted. G9a/GLP selective methyltransferase chemical probe, UNC0638. (2010). | |
| 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 | 509.7 |
| 分子式 | C30H47N5O2 |
| CAS号 | 1255580-76-7 |
| 稳定性 | ≥ 2 years |
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