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 EC 50 value of 9.5 μM. AFM-30a hydrochloride also inhibits H3 citrullination with an EC 50 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.
性状
Solid
IC50 & Target[1][2]
EC50: 9.5 μM (PAD2); 0.4 μM (H3 citrullination)
体外研究(In Vitro)
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.AFM-30a hydrochloride shows good ability to inhibit H3 citrullination with an EC50 of 0.4 μM. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay
体内研究(In Vivo)
AFM-30a hydrochloride suppresses NLRP3 signaling and decreases airway remodeling in PAD2transgenic mice. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
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)
参考文献
[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.
溶解度数据
In Vitro: H2O : 50 mg/mL (99.41 mM; Need ultrasonic)DMSO : 50 mg/mL (99.41 mM; ultrasonic and warming and heat to 60°C)配制储备液