Aminopeptidase Inhibitor

Bestatin (Standard) is the analytical standard of Bestatin. This product is intended for research and analytical applications. Bestatin is a natural, broad-spectrum, and competitive CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase inhibitor. Bestatin has anticancer effects.

L-Alanyl-L-leucine is an endogenous metabolite. This product is used for research and analytical applications. L-Alanyl-L-leucine is a competitive inhibitor of small intestinal glycyl-L-leucine hydrolase with K_i values of 0.53 mM (phosphate buffer) or 0.22 mM (Tris buffer). L-Alanyl-L-leucine can be used for research on Hartnup disease and cystinuria.

PL37 (Debio-0827) is an orally active, blood-brain barrier permeable dual enkephalinase inhibitor. PL37 inhibits aminopeptidase N, neprilysin, and metalloproteases, thereby blocking the degradation of endogenous enkephalins, elevating enkephalin levels, and activating peripheral μ- and δ-opioid receptors. PL37 induces mitochondrial dysfunction, mitophagy, and apoptosis, inhibits endothelial cell proliferation, migration, invasion, and tube formation, and suppresses hemangioma tumor growth and angiogenesis. PL37 can be used in research related to peripheral neuropathic pain, osteosarcoma-induced hyperalgesia, painful diabetic neuropathy, migraine, bone cancer pain, neuroinflammatory pain, and infantile hemangioma.

DG051 (free acid) is an effective inhibitor of leukotriene A4 hydrolase (LTA4H), with a K_d of 26 nM. It has high water solubility (greater than 30 mg/mL) and high oral bioavailability (over 80% across different species). DG051 (free acid) can be used in research related to myocardial infarction and stroke.

ST-115 is a highly potent and very specific aminopeptidase P2 inhibitor. ST-115 can be used in the research of ischemic stroke.

Puromycin aminonucleoside (Standard) is the analytical standard of Puromycin aminonucleoside. This product is intended for research and analytical applications. Puromycin aminonucleoside (NSC 3056) is the aminonucleoside portion of the antibiotic puromycin, and used in nephrosis animal models[1]. Puromycin aminonucleoside induces apoptosis[2]. Puromycin aminonucleoside is a reversible inhibitor of dipeptidyl peptidase II and cytosol alanyl aminopeptidase[3]. Puromycin aminonucleoside induces secretion of cell migrasome[4].

SDUY817 is a dual APN/NEP inhibitor, with IC₅₀ values of 0.29 μM for APN and 7.4 μM for NEP. SDUY817 exerts analgesic effects in a concentration- and time-dependent manner, and can be used for research in the field of neuropathic pain disorders.

BDM14471 is a selective inhibitor of hydroxamate aminopeptidase M1 (PfAM1), with the IC₅₀ of 6 nM.

Actinonin (Standard) is the analytical standard of Actinonin. This product is intended for research and analytical applications. 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[1][2][3][4][5].

SC-57461 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.

LTA4H-IN-3 (compound 9) is a LTA4H inhibitor with the IC₅₀ of 28 nM.

Aminopeptidase N inhibitor 1 (Compound 19b) is an aminopeptidase N inhibitor with an IC₅₀ of 25 μM. Aminopeptidase N inhibitor 1 can be used in the research of fields related to tumor angiogenesis.

LVV-hemorphin-7 is an Angiotensin IV receptor ligand and IRAP inhibitor (IC₅₀s: 17.6 nM for sheep adrenal IRAP; 5.0 nM for sheep cerebellum IRAP). LVV-hemorphin-7 inhibits the catalytic activity of IRAP. LVV-hemorphin-7 stimulates DNA synthesis. LVV-hemorphin-7 elicits a number of physiological effects, including cellular proliferation and memory enhancement.

LYRM03 is a derivative of Ubenimex (HY-B0134) and a Aminopeptidase N inhibitor. LYRM03 is isolated from Streptomyces HCCB10043. LYRM03 inhibits TLR4, MyD88, NLRP3, ASC, NF-κB and p38 MAPK, stabilizes IκB, and suppresses LPS-induced expression of iNOS and COX-2. LYRM03 reduces the levels of inflammatory cytokines and oxidative stress markers, and alleviates pulmonary edema. LYRM03 exhibits anticancer activity against breast cancer. LYRM03 has anti-inflammatory activity. LYRM03 can be used in the research of acute lung injury and breast cancer.

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.

Tyromycin A is an inhibitor targeting Leu-AP, Cys-AP and CP-A, with an IC₅₀ value of 25-41 μg/mL against porcine Leu-AP and an IC₅₀ value of 60 μg/mL against bovine CP-A. Tyromycin A inhibits the hydrolytic activity of target peptidases and exhibits selective activity against Gram-positive bacteria. Tyromycin A moderately inhibits the infectivity of HCV in human hepatocytes, with an IC₅₀ of 6.6 μM, and its inhibitory activity depends on the two maleic anhydride domains. Tyromycin A can be used in studies related to Gram-positive bacterial infections and hepatitis C virus infections.

JNJ-40929837 is a selective and orally active LTA₄H (leukotriene A₄ hydrolase) inhibitor. JNJ-40929837 effectively inhibits aminopeptidase activity and causes serum accumulation of Pro-Gly-Pro. JNJ-40929837 can be used in asthma research.

Aminopeptidase N inhibitor 2 (Compound 2k) is an APN inhibitor (IC₅₀: 4.3 μM) and has antitumor activity.

CD13-IN-1 (Compound 5f) is a CD13 inhibitor with an IC₅₀ of 1.71 μM. CD13-IN-1 can inhibit the proliferation of multiple tumor cells and has anti-tumor activity.

NI929 is a blood-brain barrier-permeable recombinant mouse aminopeptidase A (APA) inhibitor with a K_i value of 30 nM. NI929 is applicable to research on hypertension and Alzheimer's disease.