Prolyl Endopeptidase (PREP)

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.

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).

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.

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

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

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.

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.

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

Linderene acetate is a competitive inhibitor against Prolyl endopeptidase.

ONO-1603, a prolyl endopeptidase inhibitor, is used potentially for the treatment of Alzheimer's disease.

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

CGS-24592 is an orally active, selective, and potent inhibitor of neutral endopeptidase 24.11 (NEP), with an IC50 value of 1.6 nmol/L. It reduces the degradation of atrial natriuretic peptide (ANP), thereby increasing plasma ANP concentration and lowering blood pressure. CGS-24592 shows potential for research in cardiovascular diseases such as hypertension and congestive heart failure.

RB 101 suppresses enkephalinase and aminopeptidases; biologically cleaved at disulfide to produce inhibitors of both aminopeptidase N and neutral endopeptidase.

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-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-321 is an inhibitor of prolyl endopeptidase.

JTP-4819 is a potent and selective prolyl endopeptidase (PEP) inhibitor with potential for treating Alzheimer's disease. At nanomolar concentrations, it inhibited the degradation of substance P, arginine-vasopressin, and thyrotropin-releasing hormone by PEP in supernatants of the rat cerebral cortex and hippocampus. Repeated administration of JTP-4819 reversed the aging-induced decrease in brain substance P-like and thyrotropin-releasing hormone-like immunoreactivity, suggesting it may improve the imbalance of peptidergic neuronal systems that develops with senescence by inhibiting PEP activity. Additionally, JTP-4819 increased acetylcholine release from the frontal cortex and hippocampus, regions closely associated with memory, in both young and aged rats.

Kynapcin-28 is a non-competitive inhibitor of prolyl endopeptidase (PEP) with an IC50 of 76.80 μM and exhibits weak inhibitory effects on other serine proteases.

Lipohexin is a peptide antibiotic that exhibits activity against Gram-positive bacteria. It competitively inhibits human placental proline endopeptidase (proline endopeptidase) with an IC50 of 3.5 μM. Additionally, Lipohexin inhibits proline endopeptidase from Flavobacterium meningosepticum, with an IC50 of 25 μM.

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-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].

Polyozellin is a prolyl endopeptidase inhibitor with properties effective against inflammation, cancer, and diseases related to oxidative stress.

Eurystatin A is a prolyl endopeptidase inhibitor, with L-leucine and L-ornithine serving as direct precursors to the L-leucine and L-ornithine components of eurystatins A.