Prolyl Endopeptidase (PREP) Inhibitor

Salidroside (Rhodioloside) is a prolyl endopeptidase inhibitor. Salidroside alleviates cachexia symptoms in mouse models of cancer cachexia via activating mTOR signalling. Salidroside protects dopaminergic neurons by enhancing PINK1/Parkin-mediated mitophagy.

UAMC-1110 is a highly potent and selective inhibitor of fibroblast activation protein (FAP) with an IC₅₀ of 3.2 nM. UAMC-1110 also inhibits prolyl oligopeptidase (PREP) with an IC₅₀ of 1.8 μM.

KYP-2047 is a potent and BBB-penetrating prolyl-oligopeptidase (POP) inhibitor, with an K_i value of 0.023 nM. KYP-2047 reduces glioblastoma proliferation through angiogenesis and apoptosis modulation.

Pramiracetam (CI-879 free base) is a PREP (prolyl endopeptidase) inhibitor. Pramiracetam improves cognitive impairment caused by traumatic brain injury. Pramiracetam can be used in the study of neurodegenerative diseases.

Tasidotin (ILX651 free base) is a tubulin inhibitor and competitive Prolyl Endopeptidase (PREP) inhibitor, with an IC₅₀ of 10 μM against bovine tubulin. Tasidotin exhibits high cerebrospinal fluid penetration in non-human primates. Tasidotin antagonizes microtubule assembly and induces an extended assembly lag phase, thereby inhibiting mitosis and cell proliferation, and exerts cytotoxic and oncolytic effects on cancer cells. Tasidotin is metabolized into polypeptides and proline inside cells, and its in vivo metabolism is mediated by prolyl endopeptidase. Tasidotin can be applied in research related to Burkitt's lymphoma, breast cancer, leukemia, melanoma, central nervous system malignancies and various solid tumors.

Oroxylin A-7-O-glucuronide (oroxyloside) is an orally active flavonoid glucuronide and metabolite of Oroxylin A (HY-N0560). Oroxylin A-7-O-glucuronide can be extracted from the dried root of Scutellaria baicalensis. Oroxylin A-7-O-glucuronide exhibits prolyl oligopeptidase inhibitory activity. Oroxylin A-7-O-glucuronide inhibits the JNK pathway, upregulates PPARγ, and inhibits NF-κB p65 nuclear translocation. Oroxylin A-7-O-glucuronide reduces cytokine (IL-1β, IL-6) production. Oroxylin A-7-O-glucuronide exhibits anti-angiogenic, anti-tumor (glioma, liver cancer), anti-inflammatory, and hepatoprotective activities.

β-Elemonic acid is a triterpene isolated from Boswellia carterii. β-Elemonic acid induces cell apoptosis, reactive oxygen species (ROS) and COX-2 expression and inhibits prolyl endopeptidase. β-Elemonic acid exhibits anticancer and anti-inflammatory effects.

Salidroside (Standard) is the analytical standard of Salidroside. This product is intended for research and analytical applications. Salidroside (Rhodioloside) is a prolyl endopeptidase inhibitor. Salidroside alleviates cachexia symptoms in mouse models of cancer cachexia via activating mTOR signalling. Salidroside protects dopaminergic neurons by enhancing PINK1/Parkin-mediated mitophagy.

PREP inhibitor-1 (compound 27a) is a highly potent prolyl oligopeptidase (PREP) inhibitor (IC₅₀ < 1 nM).

S 17092 (S 17092-1) is an orally active cerebral prolyl-endopeptidase (PEP) inhibitor with an IC₅₀ of 1.2 nM. S 17092 inhibits cell apoptosis. S 17092 mechanism of action is to inhibit the activity of PEP, slowing down the degradation of neuroactive peptides and thus enhancing memory function. S 17092 can be used for the research of memory impairment and cognitive disorders associated with cerebral aging.

DOTA.SA.FAPi TFA is a selective FAP inhibitor with an IC₅₀ value of 0.9 nM against FAP. DOTA.SA.FAPi TFA forms stable complexes with ⁶⁸Ga and serves as a PET radiotracer for preclinical imaging of FAP-expressing tumors. DOTA.SA.FAPi TFA can be used in the research of colorectal adenocarcinoma and various other cancers.

Prolyl endopeptidase inhibitor 2 (Compound 8) was a proline endopeptidase (PEP) inhibitor with IC₅₀ value 31.11 μM. Prolyl endopeptidase inhibitor 2 can be used in the study of neurodegenerative diseases.

Prolyl Endopeptidase Inhibitor 1 (Boc-Pro-prolinal) is a potent prolyl endopeptidase (PEP; PE) inhibitor, with a K_i value of 15 nM. Prolyl Endopeptidase Inhibitor 1 has anti-amnesic effect.

Z-321 is a prolylendopeptidase (PEP) inhibitor.

BR102910 is a selective fibroblast activation protein (FAP) inhibitor with the IC₅₀ of 2 nM. BR102910 also inhibits prolyl oligopeptidase (PREP) with the IC₅₀ of 49.00 μM. BR102910 can be used for the researchof type 2

Z-Pro-Pro-CHO is a potent inhibitor of prolyl oligopeptidase (POP), with extremely high affinity for human prolyl oligopeptidase (HsPOP) (IC₅₀=0.012 μM), and it also effectively inhibits the activity of Schistosoma mansoni prolyl oligopeptidase (SmPOP) (IC₅₀=0.16 μM). Z-Pro-Pro-CHO does not block the phosphorylation of ERK or the production of TNF-α or IFN-γ in immune cells from presensitized mice, nor does it induce harmful phenotypes in cultured Schistosoma mansoni schistosomula. Z-Pro-Pro-CHO only partially inhibits epithelial cell wound healing at extremely high concentrations. Z-Pro-Pro-CHO finds wide application in studies related to schistosomiasis.

Y-29794 tosylate is a selective, orally active inhibitor for non-peptide prolyl endopeptidase (PREP), with an IC₅₀ of 3 nM and a K_i of 0.95 nM. Y-29794 tosylate enhances the effect of thyrotropin-releasing hormone (TRH) on the release of ACh in the rat hippocampus, exhibits potential neuroprotective efficacy. Y-29794 tosylate exhibits anticancer activity through inhibition of the IRS1-AKT-mTORC1 pathway. Y-29794 tosylate penetrates the brain-blood barrier (BBB).

RB 101 is a blood-brain barrier-crossing prodrug as well as aminopeptidase N and neutral endopeptidase-24.11 inhibitor. RB 101 blocks enkephalin breakdown, elevates extracellular enkephalin levels and activate δ-opioid receptor and dopamine D1 receptor. RB 101 can be used for the research of pain, depressive syndromes, and diabetic neuropathy.

Prolylisoleucine (Pro-Ile) is a dipeptide composed of Proline and Isoleucine, as well as a blocker of endopeptidase 24.16.

Z-Pro-prolinal (N-Benzyloxycarbonyl-L-prolyl-L-prolinal) is a specific, orally active prolyl endopeptidase (PREP) inhibitor with an IC₅₀ of 0.4 nM for porcine PREP.