prolyl oligopeptidase

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

Linderene acetate is a competitive inhibitor against Prolyl endopeptidase.

Leojaponin is a prolyl oligopeptidase (POP) inhibitor. Leojaponin exhibits significant cytoprotective activities against glutamate-induced toxicity at concentrations ranging from 0.1 microm to 10 microm.

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).

Corypalmine (IC50=128.0±10.5 uM) can inhibit prolyl oligopeptidase. (-)-Corypalmine shows inhibition activity against spore germination of some fungi.

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].

POP-IN-2 (Compound 7k) is a potent, covalently bound inhibitor of prolyl oligopeptidase (POP) (Ki: 6 nM).POP-IN-2 can be used in neurodegenerative disease and cancer research.

SP-13786 (UAMC-1110) is an inhibitor of fibroblast activation protein (FAP) (IC50 : 3.2 nM); also inhibits prolyl oligopeptidase (PREP) ( IC50 : 1.8 μM).

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) (Ki= 0.95 nM). Y-29794 has research value in neurodegenerative diseases and cancer.

Oroxylin A-7-O-glucuronide (Oroxylin A Glucoronide) 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.

BR103354 is a novel fibroblast activation protein (FAP) inhibitor with anti-diabetic and anti-steatotic effects. BR103354 inhibited FAP with an IC50 value of 14 nM, showing high selectivity against dipeptidyl peptidase (DPP)-related enzymes and prolyl oligopeptidase (PREP). BR103354 exhibited good pharmacokinetic properties as evidenced by oral bioavailability of 48.4% and minimal hERG inhibition. Single co-administration of BR103354 with hFGF21 reduced nonfasting blood glucose concentrations, in association with increased intact form of hFGF21 in ob/ob mice. BR103354 acts as an effective FAP inhibitor in vitro and in vivo, thereby demonstrating its potential application as an anti-diabetic and anti-NASH agent.

Buspirone (Buspirone free base) is an azaspiro compound which has a role as an anxiolytic drug, a sedative, a serotonergic agonist and an EC 3.4.21.26 (prolyl oligopeptidase) inhibitor.

Salidroside (Rhodioloside) is a bioactive phenolic glycoside compound isolated from Rhodiola crenulata. It is a prolyl endopeptidase Inhibitor.