A potent, orally active, centrally acting aminopeptidase inhibitor, the prodrug of the specific and selective aminopeptidase A inhibitor EC33.

A potent, orally available hydrophobic aminopeptidase inhibitor that structurally mimics the aminopeptidase inhibitor Tostedostat..

Beloranib is being studied as a first-in-class obesity therapy that demonstrates a unique mechanism of action through methionine aminopeptidase 2 (MetAP2 ) inhibition.

CHR-2797 is an aminopeptidase inhibitor, with IC50 values of 100 nM for LAP3 (LAP), 150 nM for PSAP (PuSA) and 220 nM for CD13 (Aminopeptidase N).

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 Ki of 0.28 nM. Actinonin also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with Ki 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.

IRAP-IN-1 is a selective insulin-regulated aminopeptidase (IRAP) inhibitor with IC50 of 32 nM, >25-fold selectivity over ERAP1 and ERAP2.IRAP-IN-1 reduces IRAP-dependent but not ERAP1-dependent cross-presentation by dendritic cells with nanomolar efficacy.

ST-115 (ST115) is a potent and specific inhibitor of aminopeptidase P2 (XPNPEP2, APP2) with IC50 of 3.7 nM.ST-115 does not inhibit ACE, neprilysin, or multiple other enzymes, and littile inhibition against Aminopeptidase P1/A/B/N (IC50=600 nM->10 uM).ST-115 can reduce bradykinin degradation, increasing its concentration and protective effects when administered intravenously at the start of reperfusion, reduced damaged area of the heart in a mouse model of myocardial infarction.In a rat model of ischemic stroke, ST-115 reduced functional deficits in a skilled walking test by 60% and reduced brain edema by 51%.ST-115 also reduced brain infarct size by 48% in a major subset of rats with small strokes.

HFI-419 is an insulin-regulated aminopeptidase (IRAP) inhibitor. HFI-419 has inhibitory potency for IRAP with Ki value of 0.48 μM. HFI-419 can be used for the research of cognitive and memory impairments such as Alzheimer's disease, brain trauma, and stroke.

BDM88951 (BDM 88951) is a highly potent, selective inhibitor of endoplasmic reticulum aminopeptidase 2 (ERAP2) with IC50 of 19 nM. BDM88951 displays selectivity index (>150) towards closely related ERAP1 and IRAP enzymes, as well as MMPs, TACE and LAP3. BDM88951 is a potent inhibitor of ERAP2-mediated hydrolysis of two nonapeptides precursors of SIINFEKL, an ovalbumine-derived antigen, in a dose dependent manner. BDM88951 engage ERAP2 in cells and inhibits antigen presentation in a cellular context, also displays favorable in vitro ADME properties and in vivo exposure.

DG013A (DG 013A) is tripeptide mimetic chemical probe (inhibitor) of ERAP1 with IC50 of 0.19 uM, 15-fold selectivity over ERAP2, potently inhibits aminopeptidase N (APN) with IC50 of 3.7 nM.