ZK 756326

ZK756326 is a nonpeptide chemokine receptor agonist for the CC chemokine receptor CCR8.

Signaling Pathways >> GPCR/G Protein >> CCR

Research Areas >> Cancer

Research Areas >> Endocrinology

Signaling Pathways >> Immunology/Inflammation >> CCR

IC50: 1.8 μM (CCR8)[1]

U87 MG cells expressing CCR8 are plated on poly-D-lysine-coated black 96-well plates at 10,000 cells/well and are cultured overnight. Cells are then loaded with Calcium 3, a Ca2+-sensitive non-wash fluorescence dye, for 60 min at 37°C in Hanks' balanced salts solution containing 20 mM HEPES, 3.2 mM CaCl2, 1% (v/v) fetal bovine serum, and 2.5 mM probenecid. Changes in intracellular free-Ca2+ concentration are measured with Fluorometric Imaging Plate Reader (FLIPR 3) immediately after the addition of agonist at room temperature. Cross-desensitization experiments are performed by a first addition of the agonist (CCL1 at 30 nM or ZK 756326 at 3 μM), immediately followed by a second addition of 100 nM CCL1[1].

[1]. Haskell CA, et al. Identification and characterization of a potent, selective nonpeptide agonist of the CC chemokine receptor CCR8. Mol Pharmacol. 2006 Jan;69(1):309-16.