AFM-30a hydrochloride

CAS: F: C24H28ClFN6O3 W: 502.97

AFM-30a hydrochloride is a potent protein arginine deiminase 2 (PAD2) inhibitor and has excellent PAD2-selectivity. AFM-

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Bioactivity	AFM-30a hydrochloride is a potent protein arginine deiminase 2 (PAD2) inhibitor and has excellent PAD2-selectivity. AFM-30a hydrochloride binds to PAD2 with an EC50 value of 9.5 μM. AFM-30a hydrochloride also inhibits H3 citrullination with an EC50 value of 0.4 μM. AFM-30a hydrochloride 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].
Target	EC50: 9.5 μM (PAD2); 0.4 μM (H3 citrullination)
Invitro	AFM-30a hydrochloride (compound 30a; 25 μM) has good potency to enter HEK293T/PAD2 cells and covalent modify PAD2 with an EC50 of 9.5 μM[1].AFM-30a hydrochloride shows good ability to inhibit H3 citrullination with an EC50 of 0.4 μM[1]. Cell Viability Assay[1] Cell Line:
In Vivo	AFM-30a hydrochloride suppresses NLRP3 signaling and decreases airway remodeling in PAD2-/-transgenic mice[2].
Name	AFM-30a hydrochloride
Formula	C24H28ClFN6O3
Molar Mass	502.97
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Reference	[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. [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.