AFM32a (PAD2-IN-1) hydrochloride, a benzimidazole-based derivative, is a potent and selective protein arginine deiminase 2 (PAD2) inhibitor. AFM32a hydrochloride shows superior selectivity for PAD2 over PAD4 (95-fold) and PAD3 (79-fold) [1].
In Vitro, In the target engagement assay, the EC 50 of AFM32a (compound 32a) hydrochloride is 8.3 μM in HEK293T/PAD2 cells, the enhanced potency of AFM32a overcomes its relatively poor ability to enter cells[1]. AFM32a (compound 32a; 1-25 μM) hydrochloride treatment strongly inhibits histone H3 citrullination with an EC 50 of 2.7 μM in HEK293T/PAD2 cells[1].
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.
In Vitro, In the target engagement assay, the EC 50 of AFM32a (compound 32a) hydrochloride is 8.3 μM in HEK293T/PAD2 cells, the enhanced potency of AFM32a overcomes its relatively poor ability to enter cells[1]. AFM32a (compound 32a; 1-25 μM) hydrochloride treatment strongly inhibits histone H3 citrullination with an EC 50 of 2.7 μM in HEK293T/PAD2 cells[1].
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.