| 货号 | 13965-25mg |
| 描述 | Protein arginine methyltransferases (PRMTs) post-translationally modify proteins, including histones, and in this way regulate gene expression, signal transduction, and protein-protein interactions.1,2 AMI-1 is a cell permeable inhibitor of PRMTs. It inhibits both yeast Type I arginine methyltransferase Hmt1p and human PRMT1 (IC50 = 3.0 and 8.8 μM, respectively).3 AMI-1 also effectively blocks the activity of PRMTs 3, 4, and 6 but not that of either SET (Sub39H1, Suv39H2, SET7) or non-SET (DOT1) lysine methyltransferases.3 The mechanism of inhibition of PRMTs by AMI-1 involves blocking peptide-substrate binding.4 AMI-1 also inhibits HIV-1 reverse transcriptase (IC50 = 5.0 μM).5 |
| 别名 | Arginine N-Methyltransferase Inhibitor-1; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Copeland, R.A.,Solomon, M.E. and Richon, V.M. Protein methyltransferases as a target class for drug discovery. Nature Reviews.Drug Discovery 8, 724-732 (2009). 2.Spannhoff, A.,Sippl, W. and Jung, M. Cancer treatment of the future: Inhibitors of histone methyltransferases. International Journal of Biochemistry and Cell Biology 41, 4-11 (2009). 3.Cheng, D.,Yadav, N.,King, R.W., et al. Small molecule regulators of protein arginine methyltransferases. The Journal of Biological Chemisty 279(23), 23892-23899 (2004). 4.Feng, Y.,Xie, N.,Wu, J., et al. Inhibitory study of protein arginine methyltransferase 1 using a fluorescent approach. Biochemical and Biophysical Research Communications 379, 567-572 (2009). 5.Skillman, A.G.,Maurer, K.W.,Roe, D.C., et al. A novel mechanism for inhibition of HIV-1 reverse transcriptase. Bioorganic Chemistry 30, 443-458 (2002). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥99% |
| 计算分子量 | 592.4 |
| 分子式 | C21H12N2O9S2 • 4Na |
| 稳定性 | ≥ 2 years |
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