Description
Cl-Amidine is an irreversible inhibitor of protein arginine deiminases (PADs; IC
50s = 0.8, 6.2, and 5.9 μM for PAD1, PAD3, and PAD4, respectively). It is cytotoxic to HL-60, MCF-7, and HT-29 cancer cells (IC
50s = 0.25, 0.05, and 1 μM, respectively). Cl-amidine (50 mg/kg) reduces
ex vivo extracellular neutrophil extracellular trap (NET) formation and increases survival in a mouse model of sepsis induced by cecal ligation and puncture (CLP). It also decreases the citrulline content in serum and joints and reduces the development of IgG autoantibodies in a mouse model of collagen-induced arthritis in a dose-dependent manner.