aminopeptidase

Aminopeptidase-IN-1 is a potent inhibitor of insulin-regulated aminopeptidase (IRAP) (Ki: 7.7 μM).Aminopeptidase-IN-1 can be used in studies of cognitive and memory disorders.

Firibastat (RB150) is a glutamyl aminopeptidase antagonist and an orally active brain penetrating prodrug of EC33. It is a first-in-class brain aminopeptidase A (APA) inhibitor with a Ki of 200 nM. Firibastat selectively and specifically inhibits conversion of brain angiotensin-II into angiotensin-III and decreases blood pressure in hypertensive rats[1][2].

Bestatin (Ubenimex) competitively inhibits many aminopeptidases, including B, N and leucine aminopeptidases. Ubenimex is a microbial metabolite and dipeptide with potential immunomodulatory and antitumor activities. Aminopeptidases has been implicated in the process of cell adhesion and invasion of tumor cells. Therefore, inhibiting aminopeptidases may partially attribute to the antitumor effect of ubenimex. This agent also activates T lymphocyte, macrophage, and bone marrow stem cell as well as stimulates the release of interleukin-1 and -2, thus further enhances its antitumor activity.

Bestatin hydrochloride (Ubenimex hydrochloride) is an inhibitor of aminopeptidase N (APN)/CD13 and aminopeptidase B.

SC-22716 is an orally active leukotriene A4 (LTA4) hydrolase inhibitor.SC-22716 has potential anti-inflammatory activity and may be used in the study of inflammatory bowel disease and psoriasis.

Methyl arachidate (Methyl Icosanoate) is an esterified form of arachidic acid

DG051 is a potent leukotriene A4 hydrolase (LTA4H) inhibitor with an IC50 of 47 nM.

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.

Puromycin aminonucleoside (NSC 3056) is an aminonucleoside antibiotic and a purine analog of puromycin. It can reversibly inhibit dipeptidyl peptidase and cytosolic alanine aminopeptidase, increase podocyte permeability by regulating ZO-1 in an oxidative stress-dependent manner, induce apoptosis, and promote the secretion of migrasomes. It is commonly used to induce nephrotic syndrome models in research.

SC 57461A is a potent and specific leukotriene A4 hydrolase (LTA4H) inhibitor.

ARM1 is a potent inhibitor of aminopeptidase and epoxide hydrolase. The IC50 values are 7.61 µM for aminopeptidase and 12.4 µM for epoxide hydrolase.

Acebilustat (CTX-4430) (ZK322) is an effective and specific leukotriene B4 hydrolase inhibitor.

Tosedostat (CHR-2797) is an orally bioavailable inhibitor of the M1 family of aminopeptidases with potential antineoplastic activity. Intracellularly converted into the poorly membrane-permeable active metabolite (CHR-79888), it inhibits puromycin-sensitive aminopeptidase (PuSA) and leukotriene A4 (LTA4) hydrolase. This inhibition in tumor cells may lead to amino acid deprivation, suppressed protein synthesis, increased proapoptotic protein Noxa levels, and ultimately, cell death.

Aminopeptidase N Ligand (CD13) NGR peptide, a polypeptide that targets CD13, functions as a carrier for mediating intracellular transmission and is commonly utilized in cancer research [1][2].

AminopeptidaseN inhibitor 2 is an APN inhibitor (IC50: 4.3 μM) with antitumor properties.

Aminopeptidase N (AP-N) inhibitor is a reversible inhibitor of AP-N/CD13 (IC50 = 25 μM). It is selective for AP-N/CD13 over matrix metalloproteinase-9 (MMP-9), angiotensin converting enzyme (ACE), neutral endopeptidase (NEP), γ-glutamyl transpeptidase, and the serine proteases dipeptidyl peptidase 4 (DPP-4) and cathepsin G at a concentration of 1 mM. AP-N inhibitor is non-cytotoxic to U937 cells at a concentration of 100 μM.

Aminopeptidase M (AMP) inhibition is of interest for several diseases, such as highly vascularized cancer types.

Leucylaminopeptidase is a metallo-peptidase that cleaves N-terminal residues from proteins and peptides. It functions as a transcription inhibitor, regulating the biosynthesis of pyrimidines, alginates, and cholera toxin, and also mediates site-specific recombination events in plasmids and bacteriophages.

α-Cyclopentyl-4-(2-quinolinylmethoxy)benzeneacetic acid was identified as possible dual inhibitors for hLTA4H and hLTC4S enzymes by the computer-aided methodology.

Bufexamac (Bufexamic acid) is a COX inhibitor for IFN-α release with anti-inflammatory, analgesic, and antipyretic action.

ecMetAP-IN-1 can be used as a QSAR model to study methionine aminopeptidase inhibitor as an anticancer agent using multiple linear regression.

Adamantanine (NSC-145160) is an amino acid transport inhibitor.

M8891 is an orally active, reversible, and brain-penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor (IC50: 54 nM; Ki: 4.33 nM). It inhibits the growth of primary endothelial cells and tumor cells, demonstrating both antiangiogenic and antitumoral activity.

TP-004 is a potent, reversible inhibitor of methionine aminopeptidase 2 (MetAP2) with an IC50 of 6 nM.