877617-45-3

中文名称 F-AMidine

英文名称 F-AMidine

CAS 877617-45-3

分子式 C14H19FN4O2

分子量 294.32

MOL 文件 877617-45-3.mol

877617-45-3 结构式

基本信息应用领域

基本信息

中文别名

化合物 T24054

英文别名

F-AMidine
N-[(1S)-1-(AMinocarbonyl)-4-[(2-fluoro-1-iMinoethyl)aMino]butyl]benzaMide

应用领域

用途1

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 m odifying 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).