peptidase

Vildagliptin (LAF237) is a cyanopyrrolidine-based, orally bioavailable inhibitor of dipeptidyl peptidase 4 (DPP-4), with hypoglycemic activity. Vildagliptin's cyano moiety undergoes hydrolysis and this inactive metabolite is excreted mainly via the urine.

Cilastatin (MK0791) is a renal dehydropeptidase-I and leukotriene D4 dipeptidase inhibitor. Since the antibiotic, IMIPENEM, is hydrolyzed by dehydropeptidase-I, which resides in the brush border of the renal tubule, cilastatin is administered with imipenem to increase its effectiveness. The drug also inhibits the metabolism of leukotriene D4 to leukotriene E4.

Dipeptidyl peptidase-IV (DPP-IV) is an enzyme that deactivates incretin hormones such as glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which are crucial in regulating blood glucose levels. Additionally, DPP-IV functions as a binding protein and ligand for various extracellular molecules. This enzyme is instrumental in research related to diabetes and cancer.

Ubiquitin Isopeptidase Inhibitor I, G5 is a caspase-independent inducer of cell necrosis that induces cell death via the death receptor pathway (IC50 of 1.76 and 1.6 μM in E1A and E1A C9DN cells, respectively).

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

Prolyl Endopeptidase Inhibitor 1 is a potent inhibitor of prolyl endopeptidase (PEP; PE)(Ki : 15 nM) , has anti-amnesic effect.

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.

Carboxypeptidase G2 (CPG2) Inhibitor (CPG2 Inhibitor) is a new CPG2 Inhibitor with antitumor activity.

AminopeptidaseN inhibitor 2 is an APN inhibitor (IC50: 4.3 μM) with antitumor properties.

Enteropeptidase fluorogenic substrate is a substrate for enteropeptidase that contains a 7-amino-4-trifluoromethylcoumarin (AFC) moiety. Enteropeptidase is a serine protease expressed in the proximal small intestine of higher animals that converts inactive trypsinogen to active trypsin by endoproteolytic cleavage. Enteropeptidase recognizes the highly specific amino acid sequence DDDDK on the fluorogenic substrate and cleaves after the lysine residue, releasing the AFC moiety. Enteropeptidase activity is quantified by fluorescent detection of AFC, which displays excitation/emission spectra of 380/500 nm.

Enteropeptidase fluorogenic substrate is a substrate for enteropeptidase that contains a 7-amino-4-trifluoromethylcoumarin (AFC) moiety. Enteropeptidase is a serine protease expressed in the proximal small intestine of higher animals that converts inactive trypsinogen to active trypsin by endoproteolytic cleavage.1,2Enteropeptidase recognizes the highly specific amino acid sequence DDDDK on the fluorogenic substrate and cleaves after the lysine residue, releasing the AFC moiety. Enteropeptidase activity is quantified by fluorescent detection of AFC, which displays excitation/emission spectra of 380/500 nm.3

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.

Human enteropeptidase-IN-1 (compound 6b) is a potent, orally active enteropeptidase inhibitor with low systemic exposure, suitable for studying anti-obesity.

Human enteropeptidase-IN-2 is a potent inhibitor of enteropeptidase (enteropeptidase) and can be used in anti-obesity studies.

Carboxypeptidase B, a peptide exonuclease, specifically degrades peptide chains by progressively hydrolyzing from the C-terminal, releasing free amino acids. It acts exclusively on peptide bonds with basic amino acids (such as arginine and lysine) at the C-terminal residues [1] [2].

Carboxypeptidase A (EC 3.4.2.1), a zinc-containing metalloprotease, catalyzes the hydrolysis of peptide bonds near the C-terminal end of polypeptides and is frequently utilized in biochemical research. As a prototypical enzyme for metalloproteases, it is essential in biological systems [1].

Carboxypeptidase C, often utilized in biochemical research, is an enzyme that excises COOH-terminal lysine, arginine, and proline, in addition to various neutral, aliphatic, aromatic, and acidic protein amino acids from peptide chains [1].

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].

Human enteropeptidase-IN-3 is an inhibitor of enteropeptidase activity, distinguished by its extended duration of inhibition, and is applicable in the research of intestinal digestive-related diseases [1].

Prolyl Endopeptidase Inhibitor 2 (Compound 8), a proline endopeptidase (PEP) inhibitor, exhibits an IC50 value of 31.11 μM. This compound is applicable in research related to neurodegenerative diseases [1].

Prolyl Endopeptidase is highly active in the brain and other tissues, where it degrades peptides containing proline, such as Substance P, neuropeptide Y, gonadotropin-releasing hormone, thyrotropin-releasing hormone, bradykinin, and angiotensin II. This enzyme is utilized in researching neuropsychiatric disorders including stress disorders, depression, and schizophrenia.

DPP-IV-IN-1 is an effective inhibitor of dipeptidyl peptidase IV (DPP-IV), a serine protease (IC50: 4.6 nM).

P32/98 hemifumarate is a dipeptidyl peptidase IV (DPP4) inhibitor with hypoglycemic properties that improves insulin sensitivity and β-cell responsiveness in the Zucker diabetic rat model, and may be useful in studies of type 2 diabetes and colitis.

Cameglipti, a dipeptidyl peptidase IV (DPP-4) inhibitor, is used potentially for the treatment of type 2 diabetes.