T-5224

Catalog No.S8966 Batch:S896604

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Technical Data

Formula

C29H27NO8
Molecular Weight 517.53 CAS No. 530141-72-1
Solubility (25°C)* In vitro DMSO 100 mg/mL (193.22 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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] View More
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 (from reference)

Cell Assay:

[1]
  • 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.
Animal Study:

[1]
  • Animal Models

    Male 8-week-old DBA/1J mice

  • Dosages

    3 mg/kg

  • Administration

    Oral gavage

Selleck's T-5224 has been cited by 15 publications

Shear Stress Drives the Cleavage Activation of Protease-Activated Receptor 2 by PRSS3/Mesotrypsin to Promote Invasion and Metastasis of Circulating Lung Cancer Cells [ Adv Sci (Weinh), 2023, 10(25):e2301059] PubMed: 37395651
c-FOS is an integral component of the IKZF1 transactivator complex and mediates lenalidomide resistance in multiple myeloma [ Clin Transl Med, 2023, 13(8):e1364] PubMed: 37581569
c-FOS is an integral component of the IKZF1 transactivator complex and mediates lenalidomide resistance in multiple myeloma [ Clin Transl Med, 2023, 13(8):e1364] PubMed: 37581569
Flubendazole inhibits PD-1 and suppresses melanoma growth in immunocompetent mice [ J Transl Med, 2023, 21(1):467] PubMed: 37452307
Flubendazole inhibits PD-1 and suppresses melanoma growth in immunocompetent mice [ J Transl Med, 2023, 21(1):467] PubMed: 37452307
Androgen Receptor/AP-1 Activates UGT2B15 Transcription to Promote Esophageal Squamous Cell Carcinoma Invasion [ Cancers (Basel), 2023, 15(24)5719] PubMed: 38136265
Diverging regulation of Bach2 protein and RNA expression determine cell fate in early B cell response [ Cell Rep, 2022, 40(1):111035] PubMed: 35793628
CPNE1 silencing inhibits cell proliferation and accelerates apoptosis in human gastric cancer [ Eur J Pharm Sci, 2022, 177:106278] PubMed: 35985444
Local administration of liposomal-based Srpx2 gene therapy reverses pulmonary fibrosis by blockading fibroblast-to-myofibroblast transition [ Theranostics, 2021, 11(14):7110-7125] PubMed: 34093874
PGE2 and thrombin induce myofibroblast transdifferentiation via activinA and CTGF in endometrial stromal cells [ Endocrinology, 2021, bqab207] PubMed: 34606582

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.