T-5224

T-5224 is an inhibitor of c-fos/activator protein 1 (AP-1). It inhibits the DNA binding activity of c-fos/AP-1 without affecting the activity of C/EBPalpha, ATF2, MyoD, Sp1, and NF-kappaB/p65 in vitro. It shows inhibitory activity in a c-fos/AP-1 promoter luciferase assay without changing c-fos family protein expression levels in TNF-alpha-stimulated NIH/3T3 cells. Administration of T-5224 (30 mg/kg) inhibits the development of collagen-induced arthritis in mice through reduction of IL-1beta production, neutrophil infiltration, and synovial cell proliferation. It reduces the inflammatory cytokine response in LPS-challenged mice, lowering levels of TNF-alpha and HMGB1 in the serum and MIP-1alpha and MCP-1 in the liver. T-5224 reduces in vivo necrosis of liver tissue and improves survival rates in LPS-challenged mice. T-5224 also exhibits anticancer activity, reducing proliferation and migration of HSC-3-M3 head and neck squamous carcinoma cells in vitro and the number of metastases in an HSC-3-M3 orthotopic xenograft model in vivo.Formal Name: 5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(2,3-dihydro-3-oxo-1,2-benzisoxazol-6-yl)methoxy]-benzenepropanoic acid. CAS Number: 530141-72-1. Molecular Formula: C29H27NO8. Formula Weight: 517.5. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml. lambdamax: 292, 332 nm. SMILES: OC1=CC(OC2CCCC2)=CC=C1C(C3=CC=C(OCC4=CC=C(C(NO5)=O)C5=C4)C(CCC(O)=O)=C3)=O. InChi Code: InChI=1S/C29H27NO8/c31-24-15-21(37-20-3-1-2-4-20)8-10-22(24)28(34)19-6-11-25(18(14-19)7-12-27(32)33)36-16-17-5-9-23-26(13-17)38-30-29(23)35/h5-6,8-11,13-15,20,31H,1-4,7,12,16H2,(H,30,35)(H,32,33). InChi Key: DALCQQSLNPLQFZ-UHFFFAOYSA-N.