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