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ERAP1 inhibitor 3

Chemical Structure : ERAP1 inhibitor 3

CAS No.: 865273-97-8

ERAP1 inhibitor 3 (ERAP1-IN-1)

Catalog No.: PC-72272Not For Human Use, Lab Use Only.

ERAP1 inhibitor 3 (ERAP1-IN-1) is a selective, small molecule inhibitor of ERAP1 with IC50 of 0.4 uM, displays no inhibitory effect against its paralogues ERAP2 and IRAP.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

ERAP1 inhibitor 3 (ERAP1-IN-1) is a selective, small molecule inhibitor of ERAP1 with IC50 of 0.4 uM, displays no inhibitory effect against its paralogues ERAP2 and IRAP.
ERAP1 inhibitor 3 allosterically activates ERAP1's hydrolysis of fluorogenic and chromogenic amino acid substrates but competitively inhibits its activity toward a nonamer peptide representative of physiological substrates.
ERAP1 inhibitor 3 inhibited antigen presentation in a cellular assay.
Compound 3 displays higher potency for an ERAP1 variant associated with increased risk of autoimmune disease.

Physicochemical Properties

M.Wt 458.452
Formula C20H21F3N2O5S
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

4-Methoxy-3-(N-(2-(piperidin-1-yl)-5-(trifluoromethyl)phenyl)sulfamoyl)benzoic acid

References

1. Zachary Maben, et al. J Med Chem. 2020 Jan 9;63(1):103-121.

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