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

LYS006 hydrochloride is a potent inhibitor of leukotriene A4 hydrolase (LTA4H) extracted from patent WO2015092740A1, example 29, has an IC50 of 2 nM. LYS006 hydrochloride can be used for the research of inflammatory and autoimmune disorders.

DG013B formate is an epimer of DG013A.

DG013B is an epimer of DG013A.

DG013A (formate) is a phosphinic acid tripeptide mimetic inhibitor. DG013A (formate) displays significantly weak affinity for both ERAP1 (IC50=33 nM) and ERAP2 (IC50=11 nM). DG013A (formate) can be used for the research of autoimmune disease and cancer.

BDM_92499 is a nanomolar selective IRAP inhibitor, with an IC50 of 3.4 nM. BDM_92499 also inhibits ERAP1 and ERAP2, with IC50 values of 0.46 μM and 4.2 μM, respectively.

Arphamenine A is an aminopeptidase B inhibitor found in Chromobacteriuin violaceum HMG361-CF4. Arphamenine A can inhibit the activity of aminopeptidase B, and can inhibit sarcoma 180 and invasive micropapillary carcinoma (IMC) cancer.

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

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.

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).

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.

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.

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.

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.

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

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

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