Aminopeptidase Inhibitor

Bestatin is a natural, broad-spectrum, and competitive CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase inhibitor. Bestatin has anticancer effects.

Puromycin aminonucleoside (NSC 3056) is the aminonucleoside portion of the antibiotic puromycin, and used in nephrosis animal models. Puromycin aminonucleoside induces apoptosis. Puromycin aminonucleoside is a reversible inhibitor of dipeptidyl peptidase II and cytosol alanyl aminopeptidase. Puromycin aminonucleoside induces secretion of cell migrasome.

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.

Bufexamac is a selective Ⅱb HDAC (HDAC6, HDAC10) and LTA4H dual inhibitor, with K_ds of 0.53 µM and 0.22 µM for HDAC6 and HDAC10. Bufexamac is a nonsteroida anti-inflammatory drug.

DG013A formate is a zinc-dependent M1-aminopeptidase inhibitor that exhibits inhibitory activity against ERAP1 (IC₅₀ = 33 nM) and ERAP2 (IC₅₀ = 11 nM). DG013A formate enhances SRHFLAFSFR epitope presentation, rescues GSW11 peptide neoantigen presentation, reduces SIINFEKL presentation, modulates the immunopeptidome, decreases HLA-B27 free heavy chain expression, and reduces IL-17A secretion. DG013A formate exhibits antiproliferative activity. DG013A formate can be used for research on autoimmune diseases and melanoma.

(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.

Sialorphin TFA is a neutral endopeptidase (NEP) and aminopeptidase N (APN) inhibitor that responds to androgen signals. Sialorphin TFA blocks the degradation of endogenous opioid peptides and interacts with μ-, δ-, κ-opioid receptors. Sialorphin TFA regulates the ERK/mTOR signaling pathway by inducing cell cycle arrest, enhancing ERK1/2 activity, and reducing the phosphorylation levels of mTOR, 4E-BP1, p70S6K; accordingly, Sialorphin TFA exhibits antiproliferative activity against colorectal cancer, glioma and prostate cancer cells without cytotoxicity. In addition, Sialorphin TFA also produces antinociceptive responses, regulates sexual behavior, relaxes corpus cavernosum smooth muscle, and alleviates experimental colitis. Sialorphin TFA is also a copper (II) ion-binding ligand. Sialorphin TFA has been used in mechanistic studies related to cancer, pain management and inflammatory bowel disease.

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.

LTA4H-IN-1 is a potent inhibitor of leukotriene A4 hydrolase (LTA4H) extracted from patent WO2015092740A1, example 29, has an IC₅₀ of 2 nM. LTA4H-IN-1 can be used for the research of inflammatory and autoimmune disorders.

SC-57461A is a potent, orally active, nonpeptide, and selective inhibitor of Leukotriene A4 (LTA4) hydrolase with IC₅₀s of 2.5 nM, 3 nM, and 23 nM for recombinant human, mouse, and rat LTA4 hydrolase, respectively.

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.

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.

Benarthin is an orally active Pyroglutamyl peptidase inhibitor, THY1 inhibitor (with a K_d value of 5.13e-08 M) and competitive PGP-1 inhibitor (K_i = 1.2 µM). Benarthin is isolated from the culture broth of Streptomyces xanthophaeus MJ244-SF1. Benarthin disrupts the THY1-SFRP1 interaction, inhibits the activation of the GSK3α/β-β-catenin pathway, and reduces the upregulation of FASLG. Benarthin attenuates urothelial anoikis and reduces cell Apoptosis. Benarthin possesses iron-chelating activity. Benarthin maintains urothelial barrier integrity and blocks the pathological cascade of renal interstitial fibroblasts induced by HAP stimulation. Benarthin can be used in studies related to kidney stones.

Psammaplin A is a marine metabolite. Psammaplin A is a selective HDAC1 (IC₅₀: 45 nM), DNA methyltransferases (IC₅₀: 18.6 nM) and aminopeptidase N (APN) (IC₅₀: 18 μM) inhibitor. Psammaplin A also inhibits DNA topoisomerase and farnesyl protein transferase. Psammaplin A is a PPARγ activator and induces apoptosis. Psammaplin A has antitumor and anti-inflammatory activities. Psammaplin A has antibacterial activity against Gram-positive bacteria and inhibits DNA synthesis and DNA gyrase activity. Psammaplin A inhibits angiogenesis.

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.