3-(5-(4-(Cyclopentyloxy)-2-hydroxybenzoyl)-2-((3-hydroxybenzo[d]isoxazol-6-yl)methoxy)phenyl)propanoicacid , ≥98% , 530141-72-1

CAS NO.：530141-72-1

Empirical Formula: C29H27NO8

Molecular Weight: 517.53

MDL number: MFCD28053483

PRODUCT Properties

• Density: 1.376±0.06 g/cm3(Predicted)
• storage temp.: Store at -20°C
• solubility: DMSO:30.5(Max Conc. mg/mL);58.93(Max Conc. mM); DMSO:PBS (pH 7.2) (1:2):0.33(Max Conc. mg/mL);0.64(Max Conc. mM); DMF:30.0(Max Conc. mg/mL);57.97(Max Conc. mM)
• form: A crystalline solid
• pka: 4.61±0.10(Predicted)
• color: White to yellow

Description and Uses

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/EBPα, ATF2, MyoD, Sp1, and NF-κB/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-α-stimulated NIH/3T3 cells. Administration of T-5224 (30 mg/kg) inhibits the development of collagen-induced arthritis in mice through reduction of IL-1β production, neutrophil infiltration, and synovial cell proliferation. It reduces the inflammatory cytokine response in LPS-challenged mice, lowering levels of TNF-α and HMGB1 in the serum and MIP-1α 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.

T-5224 is a selective activator protein-1 inhibitor that prevents lymph node metastasis in an oral cancer model.

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H302-H315-H319-H335
• Precautionary statements: P261-P280-P301+P312-P302+P352-P305+P351+P338