| 货号 | 10610-100ug |
| 描述 | Peptidyl arginine deiminase 4 (PAD4, Protein arginine deiminase 4) catalyzes the post-translational modification of arginine residues on histones to form citrulline, which plays a large role in regulating gene expression.1 Dysregulated PAD4 activity has been implicated in cancer and rheumatoid arthritis.1,2 F-Amidine inhibits PAD4 activity with an IC50 value of 21.6 μM in an in vitro activity assay.3,4 It irreversibly inactivates (kinact/KI = 3,000 M-1min-1) PAD4 by covalently modifying an active site cysteine that is important for its catalytic activity.4 F-Amidine also inhibits PAD1 and PAD3 with IC50 values of 29.5 and 350 μM, respectively.5 F-Amidine is cytotoxic to HL-60, MCF-7, and HT-29 cancer cell lines (IC50s = 0.5, 0.5 and 1 μM, respectively).6 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Jones, J.E.,Causey, C.P.,Knuckley, B., et al. Protein arginine deiminase 4 (PAD4): Current understanding and future therapeutic potential. Curr. Opin. Drug Discov. Devel. 12(5), 616-627 (2009). 2.Hill, J.A.,Southwood, S.,Sette, A., et al. Cutting edge: The conversion of arginine to citrulline allows for a high-affinity peptide interaction with the rheumatoid arthritis-associated HLA-DRB1*0401 MHC class II molecule. Journal of Immunology 171, 538-541 (2003). 3.Luo, Y.,Arita, K.,Bhatia, M., et al. Inhibitors and inactivators of protein arginine deiminase 4: Functional and structural characterization. Biochemistry 45(39), 11727-11736 (2006). 4.Luo, Y.,Knuckley, B.,Lee, Y.H., et al. A fluoroacetamidine-based inactivator of protein arginine deiminase 4: Deiminase 4: Design, synthesis, and in vitro and in vivo evaluation. Journal of the American Chemical Society 128(4), 1-9 (2006). 5.Knuckley, B.,Causey, C.P.,Jones, J.E., et al. Substrate specificity and kinetic studies of PADs 1, 3, and 4 identify potent and selective inhibitors of protein arginine deiminase 3. Biochem. 49(23), 1-28 (2010). 6.Slack, J.L.,Causey, C.P. and Thompson, P.R. Protein arginine deiminase 4: A target for an epigenetic cancer therapy. Cell Mol. Life Sci. 68(4), 709-720 (2011). | |
| 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 | 408.4 |
| 分子式 | C14H19FN4O2 • CF3COOH |
| CAS号 | 877617-46-4 |
| 稳定性 | ≥ 1 year |
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