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Y-29794 Tosylate (Y-29794) is an orally active, effective, and specific non-peptide-prolyl endopeptidase (PPCE) inhibitor.

Z-Pro-Pro-CHO acts as a prolyl oligopeptidase inhibitor with half-maximal inhibitory concentrations (IC50) of 0.16 μM for human prolyl oligopeptidase and 0.01 μM for Schistosoma mansoni prolyl oligopeptidase [1].

Z-Pro-Pro-aldehyde-dimethyl acetal is a potent prolyl endopeptidase (PREP) inhibitor, effectively impeding the activity of this cytoplasmic serine endoprotease with an IC50 of 12 nM. Its significance lies in its role in modulating cognitive dysfunction associated with aging and neurodegenerative conditions, such as Alzheimer's disease [1] [2].

Linderene acetate is a competitive inhibitor against Prolyl endopeptidase.

Salidroside is a bioactive phenolic glycoside compound isolated from Rhodiola rosea and is a prolyl endopeptidase inhibitor. Salidroside can alleviate cachexia symptoms in a tumor cachexia mouse model by activating mTOR signaling and protect dopaminergic neurons by enhancing PINK1/Parkin-mediated mitochondrial autophagy. Salidroside can also inhibit the growth of cancer cells by regulating the CDK4-cyclin D1 pathway to block the G1 phase and/or regulating the Cdc2-cyclin B1 pathway to block the G2 phase.

Oroxylin A 7-O-β-d-glucuronide and wogonoside should also be served as the chemical markers together with baicalin for the quality control of herbs and proprietary traditional Chinese medicine (PTCM) products of radix Scutellariae. Oroxylin A 7-O-glucuronide, Oroxin A, and Oroxin B can bind to the "stem" region of α-hemolysin (α-HL), when inhibiting the hemolytic activity of α-HL. Oroxylin A 7-O-glucuronide and 4', 5, 7-trihydroxy-6-methoxyflavone at a concentration of 100 microM inhibit 34 and 43% of total prolyl oligopeptidase (POP) activity, respectively.

KYP-2047 is a very potent, selective Prolyl oligopeptidase (POP) inhibitor.

BR102910 (4-Thiazolecarboxamide, N-[2-[(2S)-2-cyano-4,4-difluoro-1-pyrrolidinyl]-2-oxoethyl]-2-[(3,4-dichlorophenyl)methyl]-) is a selective inhibitor of fibroblast activated protein (FAP).

PREP inhibitor-1 is a prolyl oligopeptidase (PREP) inhibitor for the study of Alzheimer's disease.

β-Elemonic Acid (3-Oxotirucallenoic Acid) exhibits anti-inflammatory effects. Beta-Elemonic acid inhibits proliferation by inducing hypoploid cells and cell apoptosis, the anticancer effects of beta-Elemonic acid are related to the MAPK signaling pathway, ROS activation and glutathione depletion in human A549 lung cancer cells. Beta-Elemonic acid exhibits prolyl endopeptidase inhibitory activities.

Y-29794 (Compound 2) is a potent, covalent inhibitor of prolyl oligopeptidase (POP) with a Ki of 0.95 nM, holding research value in neurodegenerative diseases and cancer.

Z-Pro-prolinal (N-Benzyloxycarbonyl-L-prolyl-L-prolinal) is a specific and orally active inhibitor of prolyl endopeptidase (PREP) with an IC50 of 0.4 nM against porcine PREP [1] [2] [3].

Pramiracetam (CI-879), derived from piracetam, is a more effective nootropic drug . According to reports, Pramiracetam improved cognitive defects related with traumatic brain wounds. Pramiracetam was also potent in the therapy of cognitive disorders of traumatic origins and cerebrovascular.

Inhibitor of prolyl endopeptidase

Poststatin is a prolyl endopeptidase inhibitor produced by Streptomyces viridochromogenes MH534-30F3.

BPP is a fluorescent microviscosity probe used to image natural HOBr in living cells and zebrafish.

S 17092 (S 17092-1) is a potent inhibitor of cerebral prolyl-endopeptidase (PEP) with an IC50 value of 1.2 nM, used in research on memory impairment and cognitive disorders related to cerebral aging [1].

POP-IN-2 (Compound 7k) is a potent covalent inhibitor of prolyl oligopeptidase (POP) with a Ki of 6 nM, suitable for neurodegenerative disease and cancer research.

Z-Thioprolyl-Thioproline is a prolyl endopeptidase inhibitor derived from bovine brain, exhibiting inhibition constants of IC50 = 16 µM and Ki = 37 µM. This compound is utilized in the investigation of neurological disorders, including memory and cognitive disorders [1].

Z-Thioprolyl-Thiazolidine is a potent, specific inhibitor of bovine brain prolyl endopeptidase, demonstrating an inhibition constant (K i value) of 0.36 nM [1].

Aprepitant is a Substance P/Neurokinin-1 Receptor Antagonist. The mechanism of action of aprepitant is as a Neurokinin 1 Antagonist, and Cytochrome P450 3A4 Inhibitor, and Cytochrome P450 2C9 Inducer, and Cytochrome P450 3A4 Inducer.

gamma-preprotachykinin amide (72-92) acetate is a 21 amino acid peptide belonging to the tachykinin (TK) family and including neurokinin A (NKA) in its C-terminal sequence. gamma-preprotachykinin amide (72-92) acetate possesses higher affinity than NKA for central NK-2 receptors; it shows lower affinity for NK-1 receptors, however, it potently stimulates salivary secretion, which is mediated by NK-1 receptor activation.

Fosaprepitant dimeglumine (MK-0517) is the dimeglumine salt form of fosaprepitant, a water-soluble, N-phosphorylated prodrug of aprepitant with antiemetic activity. Upon intravenous administration and rapid conversion to aprepitant, this agent selectively binds to human substance P/neurokinin 1 (NK1) receptors in the central nervous system (CNS), inhibiting receptor binding of endogenous substance P and preventing substance P-induced emesis.

(1R,2S,3R)-Aprepitant (Compound ent-4) is a competitive antagonist of the human neurokinin-1 (NK-1) receptor. It holds potential for research in the treatment of nausea and vomiting related to cancer or postoperative conditions.