877617-45-3 Basic information More..
Product Name:F-AMidine
Synonyms:F-AMidine;N-[(1S)-1-(AMinocarbonyl)-4-[(2-fluoro-1-iMinoethyl)aMino]butyl]benzaMide;F amidine,Famidine;Benzamide, N-[(1S)-1-(aminocarbonyl)-4-[(2-fluoro-1-iminoethyl)amino]butyl]-
CAS:877617-45-3
MF:C14H19FN4O2
MW:294.32
EINECS:
Mol File:877617-45-3.mol
877617-45-3

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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).

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