Powder: -20°C for 3 years | In solvent: -80°C for 1 year
ERK5-IN-1 是 ERK5抑制剂,IC50为 87 nM。它也抑制 LRRK2[G2019S],IC50为 26 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 495 | 现货 | ||
5 mg | ¥ 1,230 | 现货 | ||
10 mg | ¥ 1,730 | 现货 | ||
25 mg | ¥ 3,180 | 现货 | ||
50 mg | ¥ 4,650 | 现货 | ||
100 mg | ¥ 6,630 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,260 | 现货 |
产品描述 | ERK5-IN-1 is a potent ERK5 inhibitor (IC50: 87 nM). It also inhibits LRRK2[G2019S] (IC50: 26 nM). |
靶点活性 | ERK5:87 nM (cell free) |
体外活性 | ERK5-IN-1能够抑制HeLa细胞中由EGF刺激的ERK5自磷酸化(EC50:0.19 μM)。 |
激酶实验 | Kinase activity was determined in an assay volume of 40 μL in kinase buffer (50 mM Tris–HCl, pH 7.5, 0.1 mM EGTA, 1 mM 2-mercaptoethanol) containing 200 ng of pure active ERK5 and the indicated amount of inhibitor. Reaction started by adding 10 mM magnesium acetate, and 50 μM [γ-32P]-ATP (500 cpm/pmol) and 250 μM PIMtide (ARKKRRHPSGPPTA) as substrates. Assays were carried out for 20 min at 30 °C, terminated by applying the reaction mixture onto p81 paper and the incorporated radioactivity measured as described previously. |
细胞实验 | HeLa cells were serum starved overnight followed by treatment with inhibitors for 1 h. Cells were then stimulated with EGF (20 ng/mL) for 17 min and harvested in RIPA buffer (1× PBS, 1% NP40, 0.5% sodium deoxycholate, 0.1% SDS, 0.1 mg/ml PMSF and 1 mM sodium orthovanadate). Proteins from total cell lysates were resolved by 6% sodium dodecyl sulfate (SDS)-poly-acrylamide gel electrophoresis (PAGE), transferred to nitrocellulose membrane, blocked in 5% nonfat milk, and blotted with anti-ERK5 antibody. |
分子量 | 459.54 |
分子式 | C25H29N7O2 |
CAS No. | 1234479-76-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 25 mg/mL (54.4 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1761 mL | 10.8804 mL | 21.7609 mL | 54.4022 mL |
5 mM | 0.4352 mL | 2.1761 mL | 4.3522 mL | 10.8804 mL | |
10 mM | 0.2176 mL | 1.088 mL | 2.1761 mL | 5.4402 mL | |
20 mM | 0.1088 mL | 0.544 mL | 1.088 mL | 2.7201 mL | |
50 mM | 0.0435 mL | 0.2176 mL | 0.4352 mL | 1.088 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
ERK5-IN-1 1234479-76-5 MAPK ERK ERK5 IN 1 Inhibitor ERK-5-IN-1 Extracellular signal regulated kinases ERK5IN1 inhibit inhibitor