| Identification | Back Directory | [Name]
F-Amidine (trifluoroacetate salt) | [CAS]
877617-46-4 | [Synonyms]
RJYLIKJNBRPBOO-MERQFXBCSA-N
F-Amidine (trifluoroacetate salt) | [Molecular Formula]
C16H20F4N4O4 | [MOL File]
877617-46-4.mol | [Molecular Weight]
408.35 |
| Hazard Information | Back Directory | [Uses]
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. Dysregulated PAD4 activity has been implicated in cancer and rheumatoid arthritis. F-amidine inhibits 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. F-amidine also inhibits PAD1 and PAD3 with IC50 values of 29.5 and 350 μM, respectively. F-amidine is cytotoxic to HL-60, MCF-7, and HT-29 cancer cell lines (IC50s = 0.5, 0.5 and 1 μM, respectively).[Cayman Chemical] | [storage]
Store at -20°C |
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