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.

Inhibitor of prolyl endopeptidase

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

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.

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].

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].

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).

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.

N-Ethylmaleimide (NEM) is a reagent for alkylation of free sulfhydryl groups, a cysteine protease inhibitor used in experimental biochemistry. N-Ethylmaleimide is also a deubiquitinating enzyme inhibitor that specifically inhibits phosphate transport in mitochondria.

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

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].