tcsc3270 FR 180204

FR 180204 is an ATP-competitive, selective ERK inhibitor with K_i of 0.31 μM and 0.14 μM for ERK1 and ERK2, respectively.

IC50 & Target: Ki: 0.31 μM (ERK1) 0.14 μM (ERK2)

In Vitro: In AP-1-transfected cells, FR180204 dose-dependently inhibits AP-1 transactivation with IC₅₀ of 3.1 μM^[1]. FR 180204 inhibits spontaneous mesothelioma cell growth^[3]. 

In Vivo: FR180204 (100 mg/kg, i.p., b.i.d.) significantly decreases the severity of symptoms and body weight loss in collagen-induced arthritis mice^[2]. In a mouse model of dengue virus (DENV) infection, FR180204 limits hepatocyte apoptosis, reduces DENV-induced liver injury, and improves clinical parameters^[4].