Protease-Activated Receptor-1 (PAR-1) Agonist, a selective peptide, activates the PAR-1 receptor by mimicking the specific actions of thrombin. It corresponds to the PAR1 tethered ligand, facilitating selective activation of this receptor.

Protease-Activated Receptor-1 (PAR-1) Agonist activates protein kinase C isoenzymes alpha and epsilon in human HT-29 colon carcinoma cells express ng PAR1 endogenously. At the cellular level, both PAR-1 Agonist and thrombin stimulate HT-29 cell migration and matrix adhesion through a PKCepsilon-dependent mechanism, as evidenced by the inhibition of PAR1-mediated effects by the PKC inhibitor bisindolylmaleimide I and the PKCepsilon translocation inhibitory peptide EAVSLKPT, but not by the PKC inhibitor Gö 6976[2].