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.

Puromycin aminonucleoside (NSC-3056) increases podocyte permeability by modulating ZO-1 in an oxidative stress-dependent manner.

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

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 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].

Betulinic acid (ALS-357) is a pentacyclic lupane-type triterpene derivative of betulin (isolated from the bark of Betula alba, the common white birch) which has antiretroviral, antimalarial, and anti-inflammatory properties, as well as a more recently discovered potential as an anticancer agent, by inhibition of topoisomerase.

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

Apstatin TFA is a potent inhibitor of aminopeptidase P (APP), with Ki values of 2.6 µM for rat APP and 0.64 µM for human APP. This compound also exhibits cardioprotective properties.

4-MDM (4-Methoxydiphenylmethane) is an orally active anti-inflammatory compound that selectively enhances the aminopeptidase activity of leukotriene A4 hydrolase (LTA4H). By promoting the degradation of proline-glycine-proline by LTA4H, 4-MDM reduces neutrophil recruitment in the lungs, alleviating inflammation without affecting the epoxide hydrolase activity of LTA4H. This compound is useful for research in pulmonary diseases.

SDUY817 is a dual APN NEP inhibitor with IC50 values of 0.29 μM for APN and 7.4 μM for NEP. It exhibits analgesic effects in a concentration- and time-dependent manner, making it a potential candidate for research in the field of neuropathic pain disorders.

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.

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

SDUY816 is an orally active dual APN NEP inhibitor, with IC50 values of 0.68 μM for APN and 6.9 μM for NEP. It exhibits analgesic properties and demonstrates good safety and pharmacokinetic profiles, having an oral bioavailability of 27% and a half-life of 4.02 hours in rats (oral, 10 mg kg). SDUY816 is applicable for research in the field of neuropathic pain disorders.

LYS006 hydrochloride is a potent inhibitor of leukotriene A4 hydrolase (LTA4H) with an IC50 value of 2 nM. It is applicable in the study of inflammatory and autoimmune diseases. For further details, please refer to compound 29 in patent document WO2015092740A1.

QGC583 is an effective and selective AminopeptidaseA (APA) inhibitor, demonstrating an IC50 of 4 nM. It inhibits APA activity in the brain, kidneys, and heart of rats.

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

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

L(+)-Leucinol is a potent inhibitor of leucine aminopeptidase.

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.

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

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.

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.

Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces and a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM. It also induces apoptosis and inhibits aminopeptidase M, aminopeptidase N, and leucine aminopeptidase, as well as MMP-1, MMP-3, MMP-8, MMP-9, and meprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin exhibits antiproliferative and antitumor activities [1][2][3][4][5].