Home Microbiology CCR agonist ZK756326 2HCl For research use only.

ZK756326 2HCl

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.

ZK756326 2HCl Chemical Structure

ZK756326 2HCl Chemical Structure

CAS: 874911-96-3

Selleck's ZK756326 2HCl has been cited by 2 publications

Purity & Quality Control

Batch: S832401 Water] 78 mg/mL] false] DMSO] 39 mg/mL] false] Ethanol] 4 mg/mL] false Purity: 99.01%
99.01

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Signaling Pathway

CCR Signaling Pathways

CCR Signaling Pathway

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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
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].
Cell Research 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.

Chemical Information & Solubility

Molecular Weight 429.38 Formula

C21H28N2O3.2HCl
CAS No. 874911-96-3 SDF Download ZK756326 2HCl SDF
Smiles C1CN(CCN1CCOCCO)CC2=CC(=CC=C2)OC3=CC=CC=C3
Storage (From the date of receipt)

In vitro
Batch:

Water : 78 mg/mL

DMSO : 39 mg/mL ( (90.82 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 4 mg/mL


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