SET7/9 SAM-Screener™ Assay Kit
货号:
600490-1920Well 基本售价:
19600.0 元 规格:
1920 wells
产品信息
概述货号 | 600490-1920Well |
描述 | Most histone lysine methyltransferases contain a conserved domain (SET) that utilizes S-adenosyl-L-methionine (SAM or AdoMet) as a co-factor to catalyze the methylation of lysine.1 SET7/9 (KMT7) is a SET domain-containing mono-methyltransferase that acts on a large number of histone and non-histone targets including histone H3, TAF10, p53, viral Tat, and estrogen receptor α.2,3 Given this broad substrate specificity, SET7/9 has important implications for a variety of human diseases, and SET7/9 has emerged as a model for studying the catalytic mechanism SET domain histone methyltransferases. This fluorescence polarization assay is based upon a proprietary small molecule fluorescent probe* that binds to the SAM binding pocket in SET7/9. Binding of the small molecule probe to SET7/9 induces an increase in fluorescence polarization. Binding of the probe can be competed with the endogenous cofactor SAM or by the inhibitor sinefungin, but is unaffected by the histone H3 peptide substrate. The SET7/9 SAM-Screener™ Assay is robust (Z’ >0.6) and exhibits a greater than 100 mP shift over a range of 0-250 nM SET7/9. The assay is suitable for high-throughput screening in the provided 384-well plate or can be scaled to higher density plate formats (e.g., 1,536-well) if desired.*United States Patent 9,120,820 |
别名 | SET7/9 SAM-Binding Site Inhibitor Screening; |
性能供应商 | Cayman |
应用文献 |
1.Bannister, A.J., and Kouzarides, T. Regulation of chromatin by histone modifications. Cell Research 21, 381-395 (2011). 2.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). 3.Dhayalan, A.,Kudithipudi, S.,Rathert, P., et al. Specificity analysis-based identification of new methylation targets of the SET7/9 protein lysine methyltransferase. Chemistry & Biology 18, 111-120 (2011).
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运输条件 | Dry ice in continental US; may vary elsewhere |
存放说明 | -80 |
稳定性 | ≥ 6 months |
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