PAD2-IN-1

Names

[ CAS No. ]:
2095109-82-1

[ Name ]:
PAD2-IN-1

Biological Activity

[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].

[Related Catalog]:

Research Areas >> Cancer

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Epigenetics >> Protein Arginine Deiminase

[Target]

Protein Arginine Deiminase 2 (PAD2)[1]

[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].

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₅H₂₉FN₆O₃

[ Molecular Weight ]:
480.53

PAD2-IN-1

Names

Biological Activity

Chemical & Physical Properties

Related Compounds