FR180204 是一种 ATP 竞争性的选择性ERK抑制剂，对ERK1和ERK2的Ki值分别为 0.31 μM 和 0.14 μM，IC50值分别为0.51 μM 和0.33 μM。

FR180204 is a potent and selective ATP-competitive inhibitor of ERK1 and ERK2.

在登革病毒（DENV）感染的小鼠模型中,FR180204限制肝细胞凋亡,减少DENV诱导的肝损伤,并改善临床参数.在胶原诱导的关节炎小鼠中,FR180204（100 mg/kg,i.p.,b.i.d.）显著降低症状和体重减轻的严重程度

FR 180204抑制自发性间皮瘤细胞生长。在AP-1转染的细胞中,FR180204剂量依赖性地抑制AP-1反式激活,IC50为3.1 μM。

ERK assay: Nunc-Immuno MaxiSorp plates are coated with 20 μg/ml MBP solution in phosphate-buffered saline (PBS). After washing with PBS containing 0.05% Tween 20 (T-PBS), blocking buffer (T-PBS containing 3% BSA) is added to each well and the plates are incubated for 10 min at room temperature. After washing with T-PBS, chemical compounds, ATP and recombinant ERK2 diluted in assay dilution buffer (20 mM Mops, pH 7.2, 25 mM β-glycerol phosphate, 5 mM EGTA, 1 mM sodium orthovanadate, 1 mM dithiothreitol, and 50 μg/ml BSA) and are added to each well. Vehicle groups (containing 0.1% DMSO) and kinase-withdrawal groups are used for the control and basal determinations. After incubation for 1 h at room temperature, plates are washed twice with T-PBS. Anti-phospho MBP antibody (0.2 μg/ml) is added to each well, and the plates are incubated for 1 h at room temperature. After washing, anti-mouse HRP-conjugated polyclonal antibodies are added and the plates were incubated for 30 min. SuperSignal chemiluminescent substrate is used for the measurement of HRP activity according to the manufacturer's instructions. Prism 4.0 software is used for the Lineweaver–Burk plot analysis, IC50 and Ki determinations.

Cell viability is assayed by the method using MTT. MTT-reactive cells are quantified at an absorbance of 570 nm using a micro-plate reader. (Only for Reference)

865362-74-9

C18H13N7

327.351

FR180204

DMSO:32.7 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years