MSX-122

For research use only. Not for use in humans.

Catalog No.S6617

MSX-122 Chemical Structure

Molecular Weight(MW): 292.34

MSX-122 is a novel small molecule and partial CXCR4 antagonist (IC50~10 nM).

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Biological Activity

Description MSX-122 is a novel small molecule and partial CXCR4 antagonist (IC50~10 nM).
Targets
CXCR4 [1]
()
~10 nM
In vitro

MSX-122 is also incapable of blocking the binding of 125I-labeled CXCL12 to CXCR4. MSX-122 appears to be insufficiently large to block all binding sites between CXCR4 and CXCL12. MSX-122 blocks certain CXCR4 functions via binding to the CXCL12-binding site and interfering with CXCR4/CXCL12-mediated signaling. MSX-122 can intervene in the Gαi-signaling pathway (cAMP modulation), but not the Gq-pathway (calcium flux)[1].

In vivo

MSX-122 blocks bleomycin-induced lung fibrosis involving chemotaxis and homing of CXCR4-positive mesenchymal progenitor cells into the lungs. MSX-122 exhibits anti-inflammatory activity in a carrageenan-induced paw edema model. MSX-122 blocks lung metastasis of breast cancer and SCCHN, and liver metastasis of uveal melanoma in vivo[1].

Protocol

Cell Research:

[1]

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  • Cell lines: MDA-MB-231 cells
  • Concentrations: 1, 10, 100, and 1000 nM
  • Incubation Time: 15 mins
  • Method:

    For binding affinity assay, MDA-MB-231 cells cultured in an 8-well slide chamber are preincubated with MSX-122 at 1, 10, 100, and 1000 nM. Then the cells are fixed with 4% formaldehyde and incubated with 50 nM biotinylated TN14003, and followed by Rhodamine staining.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: Male C57BL/6 mice (age 5–6 weeks)
  • Formulation: dissolved in 10% DMSO and 45% 2-hydroxypropyl-β cyclodextrin
  • Dosages: 10 mg/kg
  • Administration: i.p. injection
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 3 mg/mL (10.26 mM)
Water Insoluble
Ethanol 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 292.34
Formula

C16H16N6

CAS No. 897657-95-3
Storage powder
in solvent
Synonyms N/A
Smiles C(NC1=NC=CC=N1)C2=CC=C(CNC3=NC=CC=N3)C=C2

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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CXCR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID