(S)-PFI-2 (hydrochloride)
货号：
18119-1mg 基本售价：
350.0 元 规格：
1 mg
产品信息
概述| 货号 | 18119-1mg |
| 描述 | SET domain-containing protein 7/9 (SET7/9) is a histone methyltransferase that monomethylates lysine 4 of histone H3, which generates a specific tag for epigenetic transcriptional activation. It plays a role in the transcriptional activation of tumor suppressor p53 in response to DNA damage, as well as the transcription factor TAF10(Item No. 10228).1,2 (R)-PFI-2 (Item No. 14678) is a potent, cell-permeable inhibitor of SET7/9 (IC50 = 2 nM) that demonstrates greater than 1,000-fold selectivity over a panel of 18 other methyltransferases.3 (S)-PFI-2, the inactive enantiomer, is 500-fold less potent (IC50 = 1 µM) and may serve as a negative control.3 See the Structural Genomics Consortium (SGC) website for more information. |
| 别名 | (+)-PFI-2; |
性能| 供应商 | Cayman |
| 应用文献 |
1.Couture, J.F.,Collazo, E.,Hauk, G., et al. Structural basis for the methylation site specificity of SET7/9. Nature Structural & Molecular Biology 13(2), 140-146 (2006).
2.Kurash, J.K.,Lei, H.,Shen, Q., et al. Methylation of p53 by Set7/9 mediates p53 acetylation and activity in vivo. Molecular Cell 29, 392-400 (2008).
3.Barsyte-Lovejoy, D.,Li, F.,Oudhoff, M.J., et al. (R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells. Proceedings of the National Academy of Sciences of the United States of America 111(35), 12853-12858 (2014).
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| 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 | 536 |
| 分子式 | C23H25F4N3O3S • HCl |
| CAS号 | 1627607-88-8 |
| 稳定性 | ≥ 2 years |
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