ZK756326 2HCl

Catalog No.S8324

ZK756326 2HCl Chemical Structure

Molecular Weight(MW): 429.38

ZK756326 is a full agonist of CCR8(Chemokine receptor 8) with an IC50 of 1.8 μM, dose-responsively eliciting an increase in intracellular calcium and cross-desensitizing the response of the receptor to CCL1.

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Biological Activity

Description ZK756326 is a full agonist of CCR8(Chemokine receptor 8) with an IC50 of 1.8 μM, dose-responsively eliciting an increase in intracellular calcium and cross-desensitizing the response of the receptor to CCL1.
Targets
CCR8 [1]
(in U87 cell line)
1.8 μM
In vitro

ZK 756326 stimulated extracellular acidification in cells expressing human CCR8. The ability of ZK 756326 to induce a response was receptor-specific and mediated through Gαi, because it could be blocked by treatment with pertussis toxin. Like CCL1, ZK 756326 inhibited human immunodeficiency virus (HIV) fusion of cells expressing CD4 and CCR8. But unlike mCCL1, ZK 756326 bound to and activated a form of mCCR8 that was mutated to eliminate O-linked sulfation at tyrosines 14 and 15. Therefore, ZK 756326 is most probably not binding in the same manner as CCL1 but can activate the switch mechanism involved in transducing signaling events[1].

Protocol

Cell Research:

[1]

+ Expand
  • Cell lines: BW5147.3 cells
  • Concentrations: 10, 60, 400, 2400 nM
  • Incubation Time: 2 h
  • Method:

    Cells are resuspended in RPMI with 1% (w/v) BSA and 25 mM HEPES, pH 7.4 (3 × 105 cells/well), and 100-μl aliquots were loaded into upper inserts. Samples of mCCL1 and ZK 756326 prepared in 600 μl of the same medium were placed in the lower wells. After incubation (2 h at 37°C), inserts were removed, and the migrated cells were counted in an EPICS XL flow cytometer. Duplicate wells were used for each point. A migration index was established as the ratio of the number of cells that had migrated in response to the chemokine or to ZK 756326 divided by the number of cells that had migrated in response to buffer alone.


    (Only for Reference)

Solubility (25°C)

In vitro Water 78 mg/mL (181.65 mM)
DMSO 39 mg/mL (90.82 mM)
Ethanol 4 mg/mL (9.31 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 429.38
Formula

C21H28N2O3.2HCl

CAS No. 874911-96-3
Storage powder
Synonyms N/A

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CCR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID