(R)-PFI-2 (hydrochloride)
货号:
14678-25mg 基本售价:
7504.0 元 规格:
25 mg
产品信息
概述货号 | 14678-25mg |
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 TAF10.1,2 (R)-PFI-2 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 Its enantiomer, (S)-PFI-2 (Item No. 18119), is 500-fold less active (IC50 = 1 µM).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 | 1627607-87-7 |
稳定性 | ≥ 2 years |
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