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SML3778

Sigma-Aldrich

T-5224

≥98% (HPLC)

Synonym(s):

3-[5-(4-Cyclopentyloxy-2-hydroxybenzoyl)-2-[(3-oxo-1,2-benzoxazol-6-yl)methoxy]phenyl]propanoic acid, 3-{5-[4-(Cyclopentyloxy)-2-hydroxybenzoyl]-2-[(3-hydroxy-1,2-benzisoxazol-6-yl)methoxy]phenyl} propionic acid, 5-[4-(Cyclopentyloxy)-2-hydroxybenzoyl]-2-[(2,3-dihydro-3-oxo-1,2-benzisoxazol-6-yl)methoxy]benzenepropanoic acid, T 5224, T5224

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About This Item

Empirical Formula (Hill Notation):
C29H27NO8
CAS Number:
Molecular Weight:
517.53
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.21

Quality Level

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

Biochem/physiol Actions

T-5224 is an orally active, selective AP-1 transcription complex c-Fos/c-Jun inhibitor that blocks c-Fos and c-Jun DNA-binding activity, but not that of C/EBPα, ATF-2 (bZIP domain), MyoD (bHLH domain), Sp-1 (ZF domain) and NF-κB/p65 (RHD). T-5224 inhibits PMA-induced Fos/AP-1 promoter activity (IC50 ~4 μM by NIH/3T3 reporter assay) without affectingTNFα-stimulated NF-kB activity or the cellular levels of c-Fos family protein members. T-5224 exhibits therapeutic efficacy against collagen-induced arthritis (CIA) in mice in vivo (0.3-30 mg/kg/d p.o.).

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Inhibition of c-Fos expression attenuates IgE-mediated mast cell activation and allergic inflammation by counteracting an inhibitory AP1/Egr1/IL-4 axis
Journal of Translational Medicine, 19(1), 261-261 (2021)
Qian Zhao et al.
Translational oncology, 14(8), 101100-101100 (2021-05-17)
Previous studies have shown that expression of activator protein-1 (AP-1) family is significantly elevated in triple-negative breast cancer (TNBC), compared with that in other breast cancer subtypes. Here we investigated the anti-tumor effect and mechanism of T-5224, an inhibitor of
Hongjie Zhang et al.
Cardiovascular research, 119(2), 536-550 (2022-06-01)
Post-natal maturation of mammalian cardiomyocytes proceeds rapidly after birth, with most of the myocytes exiting cell cycle, becoming binucleated, and adopting oxidative phosphorylation as the primary metabolic route. The triggers and transcriptional programmes regulating cardiomyocyte maturation have not been fully
Daisuke Kamide et al.
Cancer science, 107(5), 666-673 (2016-02-27)
Activator protein-1 (AP-1) is a transcriptional factor that regulates the expression of various genes associated with tumor invasion and migration. The purpose of our study was to assess the therapeutic effects of a novel selective AP-1 inhibitor, T-5224, in preventing
c-Fos is a mechanosensor that regulates inflammatory responses and lung barrier dysfunction during ventilator-induced acute lung injury
BMC Pulmonary Medicine, 22(1), 9-9 (2022)

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