T-5224

Catalog No.S8966 Batch:S896603

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
* <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.)

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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 (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

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

References

[1] Yukihiko Aikawa, et al. Nat Biotechnol. 2008 Jul;26(7):817-23.

Selleck's T-5224 has been cited by 18 publications

Dynamic regulation of tissue fluidity controls skin repair during wound healing [ Cell, 2024, S0092-8674(24)00825-0]	PubMed: 39168124
Positive and negative feedback regulation of the TGF-β1 explains two equilibrium states in skin aging [ iScience, 2024, 27(5):109708]	PubMed: 38706856
AP-1 Mediates Cellular Adaptation and Memory Formation During Therapy Resistance [ bioRxiv, 2024, 2024.07.25.604999]	PubMed: 39091739
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

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SHIPPING AND STORAGE
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