T-5224

T-5224 is a **non-peptidic small molecule inhibitor** designed to selectively inhibit the DNA binding activity of the **c-Fos/Activator Protein-1 (AP-1)** transcription factor complex. This targeted inhibition suppresses the expression of multiple proinflammatory cytokines and matrix metalloproteinases (MMPs). T-5224 was developed with the aim of treating inflammatory disorders such as rheumatoid arthritis, osteoarthritis, and sepsis-induced acute kidney injury, as well as certain cancers. It does not affect other transcription factors such as C/EBPα, ATF-2, MyoD, Sp-1, or NF-κB. The drug was rationally designed using three-dimensional pharmacophore modeling based on the crystal structure of the AP-1–DNA complex. In preclinical studies, T-5224 demonstrated the ability to prevent joint destruction, reduce inflammation, and decrease mortality from lipopolysaccharide-induced sepsis in animal models. It also inhibits osteoclastogenesis and has shown anti-tumor effects in preclinical cancer models[1][3][4][6][8][9].

Other names

T5224T-5224T 5224R-7277R7277R 7277Benzenepropanoic acid, 5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(2,3-dihydro-3-oxo-1,2-benzisoxazol-6-yl)methoxy]-