| 名称 | FR 180204 |
| 描述 | FR 180204 is a potent and selective ATP-competitive inhibitor of ERK1 and ERK2. |
| 细胞实验 | 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) |
| 激酶实验 | 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. |
| 体外活性 | 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 |
| 体内活性 | 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。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+90% Saline : < 10 mg/mL (30.55 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : < 10 mg/mL (30.55 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.
10% DMSO+90% (20% SBE-β-CD in Saline) : < 10 mg/mL (30.55 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.
DMSO : 145 mg/mL (442.96 mM), Sonication is recommended.
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| 关键字 | Inhibitor | inhibit | FR-180204 | FR 180204 | Extracellular signal regulated kinases | ERK2 | ERK1 | ERK | Apoptosis |
| 相关产品 | Formamide | Urea | Dimethyl phthalate | Aceglutamide | Alginic acid | Cysteamine hydrochloride | Metronidazole | Sildenafil citrate | Citric Acid Triammonium | Stavudine | Gluconate Calcium | Tamoxifen |
| 相关库 | 抑制剂库 | 经典已知活性库 | 已知活性化合物库 | 自噬库 | 抗结直肠癌化合物库 | 激酶抑制剂库 | 细胞凋亡化合物库 | MAPK 抑制剂库 | 抗纤维化化合物库 | 抗衰老化合物库 | 免疫/炎症分子化合物库 | 疼痛相关化合物库 |