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Dokumente

SML3778

Sigma-Aldrich

T-5224

≥98% (HPLC)

Synonym(e):

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

Empirische Formel (Hill-System):
C29H27NO8
CAS-Nummer:
530141-72-1
Molekulargewicht:
517.53
MDL-Nummer:
MFCD28053483
UNSPSC-Code:
12352200
NACRES:
NA.21

Qualitätsniveau

100

Assay

≥98% (HPLC)

Form

powder

Farbe

white to beige

Löslichkeit

DMSO: 2 mg/mL, clear

Lagertemp.

2-8°C

Biochem./physiol. Wirkung

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.).

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable

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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
Mari Ishida et al.
Journal of intensive care, 3, 49-49 (2015-11-19)
Sepsis is a potentially fatal syndrome mediated by an early [e.g., tumor necrosis factor-alpha (TNF-α)] and late [high mobility group box-1 (HMGB-1)] proinflammatory cytokine response to infection. Sepsis-induced acute kidney injury (AKI) is associated with a high mortality. C-Fos/activator protein-1
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
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
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