prolyl oligopeptidase

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).

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.

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.

POPTc80-IN-1 (Compound LC-45) is a competitive inhibitor of Trypanosoma cruzi prolyl oligopeptidase (POPTc80), with an IC50 of 0.23 μM and a Ki of 0.054 μM. It inhibits the invasion of host cells by T. cruzi, with an IC50 of 46.71 μM.

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.

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.

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

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.

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.

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].

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.

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

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.

Linderene acetate is a competitive inhibitor against Prolyl endopeptidase.