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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 (AFM30a) 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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    Biological Activity

    PAD2 inhibitor 30a (AFM30a) 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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