ERAP1 inhibitor compound 3 allosterically activates endoplasmic reticulum aminopeptidase 1 (ERAP1) hydrolysis of fluorogenic and chromogenic amino acid substrates but competitively inhibits its activity toward a nonamer peptide representative of physiological substrates (EC50 value of 0.4 μM). ERAP1 inhibitor compound 3 inhibits ERAP1’s activity in a cellular antigen processing assay with an IC50 value of 1.0 μM.

KEYWORDS: ERAP1 inhibitor compound 3 | supplier | ERAP1 inhibitor | CAS [865273-97-8] | Peptides (Endoplasmatic reticulum) | ERAP | Inhibitor | Enzymes | ARTS1 | ALAP | ERAAP | PILS-AP | Autoimmune disease