PAD2-IN-1 hydrochloride, a benzimidazole-based derivative, is a potent and selective protein arginine deiminase 2 (PAD2) inhibitor. PAD2-IN-1 hydrochloride shows superior selectivity for PAD2 over PAD4 (95-fold) and PAD3 (79-fold).
性状
Solid
IC50 & Target[1][2]
Protein Arginine Deiminase 2 (PAD2)
体外研究(In Vitro)
In the target engagement assay, the EC 50 of PAD2-IN-1 (compound 32a) hydrochloride is 8.3 μM in HEK293T/PAD2 cells, the enhanced potency of PAD2-IN-1 overcomes its relatively poor ability to enter cells.PAD2-IN-1 (compound 32a; 1-25 μM) hydrochloride treatment strongly inhibits histone H3 citrullination with an EC 50 of 2.7 μM in HEK293T/PAD2 cells. 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.