ATI-2341

Catalog No.S8309

ATI-2341 Chemical Structure

Molecular Weight(MW): 2256.82

ATI-2341, pepducin targeting the C-X-C chemokine receptor type 4 (CXCR4), is an allosteric agonist activating the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization.

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Biological Activity

Description ATI-2341, pepducin targeting the C-X-C chemokine receptor type 4 (CXCR4), is an allosteric agonist activating the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization.
Targets
CXCR4 [1]
(in CCRF-CEM cells)
194 nM(EC50)
In vitro

ATI-2341 induces CXCR4- and G protein-dependent signaling, receptor internalization, and chemotaxis in CXCR4-expressing cells. It is the most potent agonist with an EC50 value of 194 ± 16 nM and an intrinsic activity of 81 ± 4%. ATI-2341 is a potent and efficacious mobilizer of bone marrow PMNs(polymorphonuclear neutrophils) and HSPCs(hematopoietic stem and progenitor cells) and could represent a previously undescribed therapeutic approach for the recruitment of HSPCs before ABMT(autologous bone marrow transplantation). ATI-2341 is able to induce chemotaxis of CCRF-CEM cells, inducing the typical bell-shaped curve observed with chemotactic agents[1].

In vivo Intraperitoneal (i.p.) injection of ATI-2341 in BALB/c mice results in a dose-dependent recruitment of PMNs into the peritoneum, with a maximal effect seen at 405 nmol/kg. A higher concentration of ATI-2341 results in reduced recruitment, which is reminiscent of the bell-shaped curve generally seen with chemotactic agents. Intravenous (i.v.) administration of ATI-2341 in mice results in a dose-dependent increase in PMNs in the peripheral circulation, measured 90 min after administration of compound. The effect is maximal at 0.66 μmol/kg of ATI-2341. ATI-2341 has no effect on the mobilization of lymphocytes at any dose tested[1].

Protocol

Cell Research:

[1]

+ Expand
  • Cell lines: HEK-293 cells
  • Concentrations: 0, 0.031, 0.125, 0.25, 0.5, 1 μM
  • Incubation Time: 30 min
  • Method:

    Receptors(CXCR4-eGFP) are transiently transfected into HEK-293 cells and are plated 24 h after transfection on glass coverslips coated with poly-D-lysine. The next day, cells are treated with either vehicle alone or with varying concentrations of ATI-2341 for 30 min at 37 °C followed by fixation with methanol for 5 min at −20 °C. GFP fluorescence is visualized directly using a Zeiss Axiovert inverted microscope. Images are processed using Adobe Photoshop and Adobe Illustrator.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: BALB/c mice
  • Formulation: Endotoxin-free water
  • Dosages: 300 nmol/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (44.31 mM)
Ethanol 2 mg/mL (0.88 mM)
Water Insoluble

* 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 2256.82
Formula

C104H178N26O25S2

CAS No. 1337878-62-2
Storage powder
Synonyms N/A

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CXCR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID