Drug intelligence / Profile preview

CU-CPT22

Development stage
Discontinued
Modality
Small Molecules
01

Overview

CU-CPT22 is a selective, cell-permeable small molecule inhibitor of the Toll-like receptor 1/2 (TLR1/TLR2) heterodimer complex. Developed by researchers at the University of Colorado Boulder, CU-CPT22 acts as a competitive antagonist that binds to the interfacial region of the TLR1/2 complex, preventing its heterodimerization and subsequent activation by agonists such as Pam3CSK4. By blocking TLR1/2 signaling, CU-CPT22 suppresses downstream pro-inflammatory cascades, including NF-κB activation and the production of cytokines like TNF-α and IL-1β. It has been widely utilized as a chemical probe in preclinical research to study TLR1/2-mediated inflammation in various disease models, including neurodegenerative disorders like Parkinson's disease and Alzheimer's disease, as well as vascular inflammation and cancer.

Other names
5H-Benzocycloheptene-8-carboxylic acid, 3,4,6-trihydroxy-2-methoxy-5-oxo-, hexyl esterhexyl 3,4,5-trihydroxy-2-methoxy-6-oxobenzo[7]annulene-8-carboxylate
02

Targets

TLR1TLR2 (Toll-like Receptor 2)

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