prolylendopeptidase

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.

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.

Z-321 is an inhibitor of prolyl endopeptidase.

Inhibitor of prolyl endopeptidase

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

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

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.

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

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.

S 17092 (S 17092-1) is a highly potent, reversible, and orally active small-molecule inhibitor of brain peptidylprolyl endopeptidase (PEP), with a binding constant (Ki) of 1.5 nM and an IC₅₀ of 1.2 nM against recombinant human PEP. By slowing the degradation of various neuroactive peptides, including Substance P, thyrotropin-releasing hormone (TRH), and arginine vasopressin (AVP), S 17092 increases the levels of these peptides in the brain and improves age-related or drug-induced memory and cognitive impairments in various rodent and primate animal models. S 17092 has been used in studies related to Alzheimer’s disease and cognitive impairment to evaluate the role of PEP regulation in neural function.

POP-IN-1 (Compound 12h) is an effective POP inhibitor (Ki=0.009 μM) with research potential in neurodegenerative diseases and cancer progression.

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.

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-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].

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].

SP-13786 is an inhibitor of fibroblast activation protein (FAP) and prolyl oligopeptidase (PREP) with IC50 values ​​of 3.2 nM and 1.8 μM, 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).