erap1-in-1

ERAP1-IN-1 is an endoplasmic reticulum aminopeptidase 1 (ERAP1) inhibitor that allosterically activates ERAP1's hydrolysis of fluorogenic and chromogenic amino acid substrates, while competitively inhibiting its activity toward a nonamer peptide representative of physiological substrates.

ERAP1-IN-2 (compound 3f) serves as an inhibitor for ERAP1 (endoplasmic reticulum aminopeptidase 1). The IC50 value of ERAP1-IN-2 against hERAP1 is 1.72 μM.

ERAP1-IN-3 (compound 13) is a potent inhibitor of endoplasmic reticulum aminopeptidase 1 (ERAP1), with a pIC50 value of 8.6. ERAP1-IN-3 shows potential for research in cancer immunotherapy and autoimmune disease studies.

GSK235 is an orally active and selective allosteric inhibitor of endoplasmic reticulum aminopeptidase 1 (ERAP1), boasting pIC50 values of 8.45 and 7.59 for human and murine ERAP1, respectively. It demonstrates over 1000-fold selectivity against the highly homologous enzymes ERAP2 and IRAP. GSK235 modulates the immunopeptidome of cancer cells, enhancing their antigenicity, and is applicable in colorectal cancer and arthritis research.