AFM-30a is a potent protein arginine deiminase 2 (PAD2) inhibitor and has excellent PAD2-selectivity. AFM-30a binds to PAD2 with an EC50 value of 9.5 μM. AFM-30a also inhibits H3 citrullination with an EC50 value of 0.4 μM. AFM-30a can be used for the research of certain cancers and a variety of autoimmune diseases including rheumatoid arthritis (RA), multiple sclerosis, lupus, and ulcerative colitis[1].
in vivo
AFM-30a suppresses NLRP3 signaling and decreases airway remodeling in PAD2-/-transgenic mice[2].
IC 50
PAD2
storage
Store at -20°C
References
[1] Aaron Muth, et al. Development of a Selective Inhibitor of Protein Arginine Deiminase 2. J Med Chem. 2017 Apr 13;60(7):3198-3211. DOI:10.1021/acs.jmedchem.7b00274 [2] R. Surolia, et al. Role of PAD2 Regulated Inflammasome Signaling in Arsenic Induced Airway Inflammation and Remodeling. American Journal of Respiratory and Critical Care Medicine 2020;201:A2976.