Home Proteases MMP inhibitor - Interleukins inhibitor T-5224 For research use only.

T-5224

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.

T-5224 Chemical Structure

T-5224 Chemical Structure

CAS No. 530141-72-1

Purity & Quality Control

T-5224 Related Products

Signaling Pathway

MMP Signaling Pathways

MMP Signaling Pathway

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] Click to View More Targets
In vitro
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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models Male 8-week-old DBA/1J mice
Dosages 3 mg/kg
Administration Oral gavage

Chemical Information & Solubility

Molecular Weight 517.53 Formula

C29H27NO8
CAS No. 530141-72-1 SDF --
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
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (193.22 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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

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