SLIGKV-NH2

PAR2 agonist, PAR2AP
A Potent Agonist of PAR2, Derived from PAR2 Auto-Ligand Sequence
    Cat #: GPS-100
    Alternative Name PAR2 agonist, PAR2AP
  • Lyophilized Powder
  • Bioassay Tested
  • Origin Synthetic peptide
    MW: 614.78 Da.
    Purity: >98% (HPLC)
    Effective concentration 10-250 μM.
    Sequence SLIGKV.
    Modifications Val6 - C-terminal amidation .
    Molecular formula C28H54N8O7.
    CAS No.: 190383-13-2.
    Activity SLIGKV-NH2 is a selective agonist of the Protease-activated receptor-2 (PAR2)1. The peptide is composed of the neo-N-terminal 6 amino acids of human PAR2, after receptor activation by protease cleavage1.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility Any aqueous buffer. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to one week at 4°C or three months at -20°C.
      • SLIGKV-NH2
        Alomone Labs SLIGKV-NH2 induces MAPK activation in MDA-231 cells via PAR2 activation.
        MDA-231 cells were stimulated with 10, 50 and 250 µM SLIGKV-NH2 (#GPS-100) for 15 min. Cell proteins were resolved by SDS-PAGE and probed with anti-phospho-ERK1/2.
    References - Scientific background
      • Protease-activated receptors (PARs) 1-4 belong to the superfamily of G-protein-coupled receptors (GPCRs) that are self-activated by a tethered sequence exposed by proteolysis of an extracellular domain1. PARs are activated by proteolysis in response to endogenous and exogenous proteases and can contribute to both cellular homeostasis and pathology1-2. In the case of PAR2, the exposed human peptide SLIGVK-NH2 remains tethered on the receptor and activates a primary binding site located on second loop of the receptor1. As an obvious consequence of its activation mechanism, PAR2 is associated with pathologies with a strong protease release. The involvement of PAR2 in inflammatory diseases such as arthritis, lung inflammation (asthma), inflammatory bowel disease, sepsis, and pain disorders4-6 makes PAR2 an attractive target for drug intervention3. The extracellular N-terminus of PAR2 (46 residues long) contains a putative trypsin cleavage site R34 and S351, followed by LIGKV. The human-derived SLIGKV-NH2 is a small peptide that mimics the ligand binding properties of the tethered ligand exposed by proteolysis of the N-terminus from the natural receptor7 and hence, a significant tool used to study PAR2.
    Net Peptide Content: 100%
    Last update: 21/11/2019

    SLIGKV-NH2 (#GPS-100) is a highly pure, synthetic, and biologically active peptide.

    For research purposes only, not for human use
    Citations
      • Fujii, N. et al. (2017) Exp. Physiol. 102, 265.
      • Jia, X. et al. (2014) FEBS Lett. 588, 3047.
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