T-5224

T-5224 is a transcription factor c-Fos/activator protein (AP) -1 inhibitor with anti-inflammatory effects, which specifically inhibits the DNA binding activity of c-Fos/c-Jun without affecting other transcription factors. T-5224 inhibits the IL-1β-induced up-regulation of Mmp-3, Mmp-13 and Adamts-5 transcription[1][2].

Product Specifications

CAS Number

[530141-72-1]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

AP-1; MMP

Type

Reference compound

Related Pathways

Immunology/Inflammation; Metabolic Enzyme/Protease

Field of Research

Others

Assay Protocol

https://www.medchemexpress.com/T-5224.html

Purity

99.59

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

OC1=NOC2=CC(COC3=C(CCC(O)=O)C=C(C(C4=C(O)C=C(OC5CCCC5)C=C4)=O)C=C3)=CC=C21

Molecular Formula

C29H27NO8

Molecular Weight

517.53

Precautions

H302, H315, H319, H335

References & Citations

[1]Makino H, et al. A selective inhibition of c-Fos/activator protein-1 as a potential therapeutic target for intervertebraldisc degeneration and associated pain. Sci Rep. 2017 Dec 5;7 (1) :16983.|[2]Aikawa Y, et al. Treatment of arthritis with a selective inhibitor of c-Fos/activator protein-1. Nat Biotechnol. 2008 Jul;26 (7) :817-23.|[3]Kamide D, et al. Selective activator protein-1 inhibitor T-5224 prevents lymph node metastasis in an oral cancer model. Cancer Sci.?2016 May;107 (5) :666-73.|[4]Izuta S, et al. T-5224, a selective inhibitor of c-Fos/activator protein-1, attenuates lipopolysaccharide-induced liver injury in mice. Biotechnol Lett. 2012 Dec;34 (12) :2175-82.|[5]Uchihashi S, et al. Metabolism of the c-Fos/activator protein-1 inhibitor T-5224 by multiple human UDP-glucuronosyltransferase isoforms. Drug Metab Dispos. 2011 May;39 (5) :803-13.|[6]Miyazaki H, et al. The effects of a selective inhibitor of c-Fos/activator protein-1 on endotoxin-induced acute kidney injury in mice. BMC Nephrol. 2012 Nov 23;13:153.