FR 180204

Description	in vitro: FR180204 inhibited the kinase activity of ERK1 and ERK2, with K(i) values 0.31 and 0.14microM, respectively. Lineweaver-Burk analysis of the binding interaction revealed that FR180204 acted as competitive inhibitor of ATP. In mink lung epithelial Mv1Lu cells, FR180204 inhibited TGFbeta-induced luciferase-expression. Discovered by Ohori and co-workers, it has IC50 values of 0.51 and 0.33 μM in enzymatic assays against ERK1 and ERK2, respectively. It was also shown to inhibit TGFβ-induced AP-1 activation with an IC50 of 3.1 μM in a cellular assay . in vivo: Preventive administration of FR180204 (100 mg/kg, i.p., b.i.d.) significantly ameliorated the clinical arthritis and body weight loss occurring in the CIA mice. Further, FR180204-treated mice showed a significant decrease in plasma anti-CII antibody levels (62%). FR180204 also attenuated delayed-type hypersensitivity in CII-immunized DBA/1 mice, an inflammatory response elicited by CII-reactive T cells, in a dose-dependent m
Pathways	MAPK Pathway
Targets	MEK/ERK

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