erap1

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 modulator-1 (Compound 1) is a regulator of endoplasmic reticulum aminopeptidase 1 (ERAP1) with an IC50 of less than 250 nM.

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.

ERAP1 modulator-2 (compound 10) is a potent ERAP1 inhibitor with an IC50 value of less than 100 nM.

DG013A (formate) is a tripeptide-mimicking inhibitor of hypophosphorous acid. It exhibits IC50 values of 33 nM for ERAP1 and 11 nM for ERAP2. This compound can be utilized in research related to autoimmune diseases and cancer.

BDM_92499 is a nanomolar, selective IRAP inhibitor with an IC50 of 3.4 nM. It also inhibits ERAP1 and ERAP2, with IC50 values of 0.46 μM and 4.2 μM, respectively.

DG026 is a IRAP inhibitor. DG026 ables to selectively downregulate IRAP-dependent cross-presentation by dendritic cells but leave ERAP1-dependent cross-presentation unaffected.

DG013A is a mimetic inhibitor of hypophosphonic acid tripeptides, capable of acting on ERAP1 (IC50: 33 nM) and ERAP2 (IC50: 11 nM).DG013A can be used to study autoimmune diseases and cancer.

DG046 is a novel potent phosphinic pseudopeptide ERAP1 inhibitor, binding in the ERAP1 active site, being stabilized by an unusual extensive network of π-stacking interactions