Aminopeptidase Inhibitor

Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase. Actinonin is a potent reversible peptide deformylase (PDF) inhibitor with a K_i of 0.28 nM. Actinonin also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with K_i values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin is an apoptosis inducer. Actinonin has antiproliferative and antitumor activities.

Tosedostat (CHR-2797) is an orally active aminopeptidase inhibitor. CHR-2797 exerts antiproliferative effects against a range of tumor cell lines.

ERAP1-IN-1 is an endoplasmic reticulum aminopeptidase 1 (ERAP1) inhibitor. ERAP1-IN-1 competitively inhibits ERAP1 activity towards a nonamer peptide representative of physiological substrates.

TNP-470 is a methionine aminopeptidase-2 inhibitor and also an angiogenesis inhibitor.

Amastatin hydrochloride is a slow, tight binding, competitive aminopeptidase (AP) inhibitor with K_i values of 0.26 nM, 30 nM, 52 nM for Aeromonas aminopeptidase, cytosolic leucine aminopeptidase, microsomal aminopeptidase.

ERAP1-IN-4 is an orally acvtive endoplasmic reticulum aminopeptidase 1 (ERAP1) inhibitor with a pIC₅₀ of 7.9 and an LLE of 5.3. ERAP1-IN-4 inhibits hydrolysis of peptide substrates by ERAP1, with high activity against Allotype1 and Allotype2. ERAP1-IN-4 reduced efficacy against other allotypes, and modulates ERAP1-mediated peptide processing to inhibit antigenic epitope presentation. ERAP1-IN-4 can be used for the research of cancer^[1].

Firibastat (QGC001), an orally active brain penetrating proagent of EC33, is a first-in-class brain aminopeptidase A (APA) inhibitor (K_i=200 nM). Firibastat selectively and specifically inhibits conversion of brain angiotensin-II into angiotensin-III and decreases blood pressure in hypertensive rats.

β-Spaglumic acid (β-NAAG) is a competitive NAAG peptidase inhibitor (K_i=1 µM) that protects spinal cord neurons from excitotoxicity and hypoxic damage. β-Spaglumic acid is also a selective mGluR3 antagonist (mGluR3 receptor functions to regulate activity-dependent synaptic potentiation in the hippocampus). β-Spaglumic acid can be used in neuroprotection-related studies.

Acebilustat (CTX-4430) is a leukotriene A4 hydrolase inhibitor, used for an oral antiinflammatory agent.

L-Leucinol ((+)-Leucinol) is a competitive aminopeptidase inhibitor with a K_i value of 17 μM. As a dietary intake inhibitor, L-Leucinol reduces the basal dietary leucine intake in rats via microinjection into the rat anterior piriform cortex.

Aminopeptidase-IN-1 is an insulin-regulated aminopeptidase (IRAP) inhibitor with an K_i value of 7.7 μM. Aminopeptidase-IN-1 can be used for the research of memory impairments.

ERAP2-IN-1 (compound 61) is an uncompetitive ERAP2 inhibitor. ERAP2-IN-1 specifically inhibits the ERAP2 peptide hydrolysis activity, inhibiting Arg-AMC hydrolysis with an IC₅₀ of 27 μM and model peptide hydrolysis with an IC₅₀ of 44 μM.

Apstatin TFA is a potent aminopeptidase P (APP) inhibitor with K_i values of 2.6, 0.64 µM for rat and human APP, respectively. Apstatin TFA shows cardioprotection.

HFI-142 is an insulin-regulated aminopeptidase (IRAP) inhibitor with a K_i of 2.01 μM.

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

HFI-437 is a potent non-peptidic insulin-regulated aminopeptidase (IRAP) inhibitor with a K_i of 20 nM. HFI-437 is a cognitive enhancer.

ARM1 (4BSA) is a potent aminopeptidase and epoxide hydrolase inhibitor. ARM1 shows aminopeptidase inhibitory activity with an IC₅₀ 7.61 µM and epoxide hydrolase inhibitory activity with an IC₅₀ 12.4 µM.

(rac)-BDM88951 is the racemate of BDM88951 (HY-176778). BDM88951 (Compound 4 d) is a selective ERAP2 inhibitor with an IC₅₀ of 19 nM. BDM88951 significantly inhibits antigen presentation in HEK cells. BDM88951 can be used for research on autoimmune diseases and cancer.

Methyl arachidate (Methyl icosanoate) is a component of lipid mixtures. Methyl arachidate can be isolated from flowering plants. Methyl arachidate inhibits LTA4H. Methyl arachidate shows no antifeedant activity against Leptinotarsa decemlineata.

2-(2’-Pyridyl)benzimidazole is a potentially tridentate ligand that can form stable complexes with various transition metal ions. 2-(2’-Pyridyl)benzimidazole can be used as an anti-inflammatory agent and an inhibitor of Escherichia coli methionine aminopeptidase.