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T-5224

For research use only.

Catalog No.S8966

4 publications

T-5224 Chemical Structure

CAS No. 530141-72-1

T-5224 is a selective inhibitor of transcription factor c-Fos/activator protein (AP)-1 with anti-inflammatory effects. T-5224 specifically inhibits the DNA binding activity of c-Fos/c-Jun and the IL-1β-induced up-regulation of Mmp-3, Mmp-13 and Adamts-5 transcription.

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Selleck's T-5224 has been cited by 4 publications

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Choose Selective MMP Inhibitors

Biological Activity

Description T-5224 is a selective inhibitor of transcription factor c-Fos/activator protein (AP)-1 with anti-inflammatory effects. T-5224 specifically inhibits the DNA binding activity of c-Fos/c-Jun and the IL-1β-induced up-regulation of Mmp-3, Mmp-13 and Adamts-5 transcription.
Targets
c-Fos/AP-1 [1]
()
c-Jun [1]
()
IL-1β [1]
()
MMP-3 [1]
()
MMP-13 [1]
()
In vitro

T-5224 inhibits matrix-degrading MMPs and inflammatory cytokines including interleukin 1β. T-5224 reduces the amounts of inflammatory cytokines and MMPs in vitro in synovial cell and chondrocyte cultures.[1]

In vivo

T-5224 is an inhibitor of c-Fos/activator protein-1 (AP-1) that prevents type II collagen–induced arthritis by reducing the amounts of inflammatory cytokines, MMPs and anti-tumor necrosis factor α in vivo in sera and joints.[1]

Protocol

Cell Research:

[1]

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  • Cell lines: NIH/3T3, RAW264.7, human synovial sarcoma SW982 and human chondrosarcoma SW1353 cells
  • Concentrations: 5.2 μM, 10 μM, 17 μM, 30 μM, 14 μM, 20 μM, 28 μM, 40 μM, 57 μM, 80 μM
  • Incubation Time: 1 h
  • Method:

    Reporter assay. NIH/3T3 cells are transiently transfected with the luciferase reporter plasmids pAP-1-Luc(×7 TGACTAA), pNF-kB-Luc(×5 TGGGGACTTTCCGC) or control phRL-TK, and cultured overnight. Cells are incubated in 0.5% FBS/DMEM containing T-5224 for 1 h, and then stimulated with PMA (10 ng/ml) or TNFa (10 ng/ml), and then cultured for 3 h, followed by measurement of lysate by using dual-luciferase reporter assay system.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: Male 8-week-old DBA/1J mice
  • Dosages: 3 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (193.22 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 517.53
Formula

C29H27NO8

CAS No. 530141-72-1
Storage powder
in solvent
Synonyms N/A
Smiles C1CCC(C1)OC2=CC(=C(C=C2)C(=O)C3=CC(=C(C=C3)OCC4=CC5=C(C=C4)C(=O)NO5)CCC(=O)O)O

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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.

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MMP Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID