tcsc3190 T-5224

T-5224 is a selective inhibitor of c-Fos/activator protein (AP)-1 for rheumatoid arthritis therapy, and inhibits MMP activity with IC₅₀s of 10 nM for both MMP-3 and MMP-13.

IC50 & Target: IC50: 10 nM (MMP-3), 10 nM (MMP-13)

In Vitro: T-5224 (0-80 μM) significantly inhibits the invasion, migration, and MMP activity of HSC-3-M3 cells in a dose-dependent manner. There is no significant influence on HSC-3-M3 amd OSC-19 cells proliferation^[4].

In Vivo: G2 is observed in rat and monkey liver microsomes as a major metabolite of T-5224, suggesting that G2 is not a human-specific metabolite^[1]. T-5224 (300 mg/kg, p.o.) inhibits the production of TNF-alpha and other downstream effectors in C57BL/6 mice^[2]. Administration of T-5224 (300 mg/kg, p.o.) after intraperitoneal injection of LPS impartes appreciable protection against acute elevations in serum levels of TNFα, HMGB1, ALT/AST as well as in liver tissue levels of MIP-1α and MCP-1, and reduces the lethality (27%)^[3].