产品编号：F101250

产品规格：25mg

产品价格：面议

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产品详情

标准品编号:	F101250
名称:	F-Amidine
别名:	N-[(1S)-1-(Aminocarbonyl)-4-[(2-fluoro-1-iminoethyl)amino]butyl]benzamide;
CAS号:	877617-45-3
参考CAS:	877617-46-4 TFA salt
分子式:	C₁₄H₁₉FN₄O₂
分子量:	294.32
种类:	Research Tools;
应用:	An inhibitor of Peptidyl arginine deiminase 4 (PAD4) activity with an IC50 value of 21.6 μM in an in vitro activity assay. 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. Dysregulated PAD4 activity has been implicated in cancer and rheumatoid arthritis. F-amidine also inhibits PAD1 and PAD3 with IC50 values of 29.5 and 350 μM, respectively. F-amidine is cytotoxic to HL-60, MCF7 and HT-29 cancer cell lines (IC50s = 0.5, 0.5 and 1 μM, respectively).
参考文献	Jones, J.E. et al.: Curr. Opin. Drug Discov. Dev., 12, 616 (2009); Hill, J.A. et al.: J. Immunol., 171, 538 (2003); Luo, Y. et al.: Biochemistry, 45, 11727 (2006); Knuckley, B. et al.: Biochemistry, 49, 1 (2010); Slack, J.L. et al.: Cell. Mol. Life Sci., 68, 709 (2011);