Aminopeptidase Inhibitor

LTA4H-IN-4 (compound 3) is an orally active LTA4H inhibitor. The IC₅₀ value of LTA4H-IN-4 for hERG is 156 μM. LTA4H-IN-4 can be used in inflammation related studies.

ERAP1-IN-3 (compound 13) is a potent endoplasmic reticulum aminopeptidase 1 (ERAP1) inhibitor, with a pIC₅₀ of 8.6. ERAP1-IN-3 has potential for the research of cancer immunotherapy and autoimmune disease.

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

Lanopepden camsylate (GSK1322322 camsylate) is a high-affinity bacterial peptide deformylase inhibitor. Lanopepden camsylate is applicable to research related to bacterial infections.

GSK235 is an orally active, selective and allosteric endoplasmic reticulum aminopeptidase 1 (ERAP1) inhibitor with pIC₅₀ values of 8.45 and 7.59 for human and mouse ERAP1, respectively. GSK235 exhibits over 1000-fold selectivity for the two most homologous enzymes, ERAP2 and IRAP. GSK235 can regulate the immunopeptidome of cancer cells and enhance cancer cell antigenicity. GSK235 can be used for the study of colorectal cancer and arthritis.

Cyanostatin B, a cyanobacterial lipopeptide, is a leucine aminopeptidase M (LAP) inhibitor (IC₅₀ = 12 ng/mL). Cyanostatin B is a weak inhibitor of protein phosphatase (PP2A) and also exhibits weak inhibitory activity against angiotensin-converting enzyme (ACE), with an IC₅₀ value of 130 μg/mL. Cyanostatin B demonstrates both cytotoxic and genotoxic effects on human hepatocytes, although non-toxic to Artemia salina. Cyanostatin B inhibits the proliferation of HepG2 cells, induces DNA single-strand breaks, and causes genomic instability..

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.

Methyl arachidate (Standard) is the analytical standard of Methyl arachidate (HY-W004291). This product is intended for research and analytical applications. Methyl arachidate (Methyl icosanoate) is a component of lipid mixtures. Methyl arachidate can be isolated from flowering plants. Methyl arachidate inhibits LTA4H. Methyl arachidate shows no antifeedant activity against Leptinotarsa decemlineata.

LTA4H-IN-5 (Compound H122) is an orally active inhibitor for leukotriene A4 hydrolase (LTA4H), that inhibits the LTA4H aminopeptidase and LTA4H hydrolase with IC₅₀ of 0.38 nM and 16.93 nM. LTA4H-IN-5 exhibits good pharmacokinetic characteristics in C57 mice and ameliorates the DNBS-induced ulcerative enteritis in rat models.

Bufexamac (Standard) is the analytical standard of Bufexamac. This product is intended for research and analytical applications. Bufexamac is a selective Ⅱb HDAC (HDAC6, HDAC10) and LTA4H dual inhibitor, with Kds of 0.53 μM and 0.22 μM for HDAC6 and HDAC10. Bufexamac is a nonsteroida anti-inflammatory drug.

Bestatin (hydrochloride) (Standard) is the analytical standard of Bestatin (hydrochloride). This product is intended for research and analytical applications. Bestatin hydrochloride is an inhibitor of CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase, used for cancer research.

Sialorphin is a neutral endopeptidase (NEP) and aminopeptidase N (APN) inhibitor that responds to androgen signals. Sialorphin blocks the degradation of endogenous opioid peptides and interacts with μ-, δ-, κ-opioid receptors. Sialorphin regulates the ERK/mTOR signaling pathway by inducing cell cycle arrest, enhancing ERK1/2 activity, and reducing the phosphorylation levels of mTOR, 4E-BP1, p70S6K; accordingly, Sialorphin exhibits antiproliferative activity against colorectal cancer, glioma and prostate cancer cells without cytotoxicity. In addition, Sialorphin also produces antinociceptive responses, regulates sexual behavior, relaxes corpus cavernosum smooth muscle, and alleviates experimental colitis. Sialorphin is also a copper (II) ion-binding ligand. Sialorphin has been used in mechanistic studies related to cancer, pain management and inflammatory bowel disease.

JNJ-26993135 is a selective leukotriene A4 hydrolase (LTA4H) inhibitor with the IC₅₀ value of 11 nM.

Probestin is a potent aminopeptidase N (APN) inhibitor produced by Streptomyces cyanogens MH663-2F6.

DG013A is a zinc-dependent M1-aminopeptidase inhibitor that exhibits inhibitory activity against ERAP1 (IC₅₀ = 33 nM) and ERAP2 (IC₅₀ = 11 nM). DG013A enhances SRHFLAFSFR epitope presentation, rescues GSW11 peptide neoantigen presentation, reduces SIINFEKL presentation, modulates the immunopeptidome, decreases HLA-B27 free heavy chain expression, and reduces IL-17A secretion. DG013A exhibits antiproliferative activity. DG013A can be used for research on autoimmune diseases and melanoma.

SC-22716 is a potent, competitive, reversible inhibitor of human LTA₄ hydrolase, with an IC₅₀ of 0.20 µM. SC-22716 has potential for the research of inflammatory bowel disease (IBD) and psoriasis.

Leuhistin is an AP-M (aminopeptidase-M) inhibitor. AP-M is an inactivating enzyme of bioactive peptides in cerebral membranes. Leuhistin can be produced by Bacillus laterosporus BMI156-14F1.

IRAP-IN-1 (compound 3) is a potent and selective insulin regulated aminopeptidase (IRAP) inhibitor with an IC₅₀ value of 157 nM.

HFI-142 (Standard) is the analytical standard of HFI-142 (HY-110259). This product is intended for research and analytical applications. HFI-142 is an insulin-regulated aminopeptidase (IRAP) inhibitor with a K_i of 2.01 μM.

Firibastat (Standard) is the analytical standard of Firibastat. This product is intended for research and analytical applications. Firibastat (QGC001), an orally active brain penetrating proagent of EC33, is a first-in-class brain aminopeptidase A (APA) inhibitor (Ki=200 nM). Firibastat selectively and specifically inhibits conversion of brain angiotensin-II into angiotensin-III and decreases blood pressure in hypertensive rats.