SML3778
T-5224
≥98% (HPLC)
别名:
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
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生化／生理作用
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.).
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
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)
Yukihiko Aikawa et al.
Nature biotechnology, 26(7), 817-823 (2008-07-01)
To inhibit arthritis upstream of inflammatory cytokine release and matrix metalloproteinase (MMP) action, we designed de novo a small-molecule inhibitor of c-Fos/activator protein-1 (AP-1) using three-dimensional (3D) pharmacophore modeling. This model was based on the 3D structure of the basic
Yohan Choi et al.
Endocrinology, 162(9) (2021-06-26)
FOS, a subunit of the activator protein-1 (AP-1) transcription factor, has been implicated in various cellular changes. In the human ovary, the expression of FOS and its heterodimeric binding partners JUN, JUNB, and JUND increases in periovulatory follicles. However, the
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
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)
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