This product is freeze dried. All water molecules have been removed.
Every lot is tried & tested in a relevant biological assay.
Ossovskaya V. S. and Bunnett N. W. (2004) Physiol. Rev. 84, 579.
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.
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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.
SLIGKV-NH2 (#GPS-100) is a highly pure, synthetic, and biologically active peptide.