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 valu
In Vitro:AFM-30a hydrochloride (compound 30a; 25 μM) has good potency to enter HEK293T/PAD2 cells and covalent modify PAD2 with an EC 50 of 9.5 μM. AFM-30a hydrochloride shows good ability to inhibit H3 citrullination with an EC 50 of 0.4 μM. MCE has not
In Vivo:AFM-30a hydrochloride suppresses NLRP3 signaling and decreases airway remodeling in PAD2 -/- transgenic mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Biological Activity: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 valu