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Chemical Structure : ERAP1 inhibitor 3
Catalog No.: PC-72272Not For Human Use, Lab Use Only.
ERAP1 inhibitor 3 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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ERAP1 inhibitor 3 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.
| M.Wt | 458.452 | |
| Formula | C20H21F3N2O5S | |
| Appearance | Solid | |
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1. Zachary Maben, et al. J Med Chem. 2020 Jan 9;63(1):103-121.
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