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PAD2 inhibitor 30a

Chemical Structure : PAD2 inhibitor 30a

CAS No.: 2095107-57-4

PAD2 inhibitor 30a (AFM30a)

Catalog No.: PC-20327Not For Human Use, Lab Use Only.

PAD2 inhibitor 30a is a potent, selective protein arginine deiminase 2 (PAD2) inhibitor with IC50 of EC50 of 9.5 uM in target engagement assays in HEK293/PAD2 cells.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

PAD2 inhibitor 30a is a potent, selective protein arginine deiminase 2 (PAD2) inhibitor with IC50 of EC50 of 9.5 uM in target engagement assays in HEK293/PAD2 cells.
PAD2 inhibitor 30a displays good selectivity for PAD2 (1.6-fold over PAD1, 47-fold over PAD3 and ~15-fold over PAD4), based on kinact/KI values.
PAD2 inhibitor 30a is a 12–50-fold more potent PAD2 inhibitors than BB-Clamidine in vitro.
PAD2 inhibitor 30a inhibits H3 citrullination in HEK293T/PAD2 cells with EC50 of 0.4 uM, >30-fold less cytotoxic than BB-Cl-amidine.
PAD2 inhibitor 30a is a powerful tool for validating the therapeutic relevance of inhibiting PAD2 in multiple disease states, i.e., breast cancer, multiple sclerosis and rheumatoid arthritis.

Physicochemical Properties

M.Wt 466.52
Formula C24H27FN6O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-N-(4-(2-fluoroacetimidamido)-1-(4-methoxy-1-methyl-1H-benzo[d]imidazol-2-yl)butyl)-3-oxoisoindoline-4-carboxamide

References

1. Muth A, et al. Development of a Selective Inhibitor of Protein Arginine Deiminase 2.. J Med Chem. 2017.

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