Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BIX02189 是一种选择性 MEK5 抑制剂,IC50 为 1.5 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 341 | 现货 | ||
2 mg | ¥ 532 | 现货 | ||
5 mg | ¥ 747 | 现货 | ||
10 mg | ¥ 1,330 | 现货 | ||
25 mg | ¥ 2,490 | 现货 | ||
50 mg | ¥ 3,990 | 现货 | ||
100 mg | ¥ 5,890 | 现货 | ||
200 mg | ¥ 7,960 | 现货 | ||
500 mg | ¥ 11,800 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 822 | 现货 |
产品描述 | BIX02189 is a selective inhibitor of MEK5 with IC50 of 1.5 nM. |
靶点活性 | MEK5:1.5 nM |
体内活性 | 用BIX02189预处理以剂量依赖性方式抑制山梨醇诱导的HeLa细胞中ERK5的磷酸化,并且对ERK1/2,p38和JNK1/2 MAPKs的磷酸化没有抑制活性。在HeLa或HEK293细胞中仅用BIX02189处理24小时不显示任何细胞毒性作用。BIX02189抑制HeLa和HEK293细胞中MEK5/ERK5/MEF2C驱动的萤光素酶表达,IC50分别为 0.53 μM和0.26 μM。BIX02189抑制MEK5和ERK5催化活性,IC50分别为1.5 nM和59 nM。BIX02189抑制CSF1R(FMS),IC50为46 nM,但对相关激酶MEK1,MEK2,ERK1,p38α,JNK2,EGFR和STK16无活性,IC50 >3.7 μM。BIX02189增强山梨醇诱导的NRCM细胞凋亡,证实了ERK5在心肌细胞中的保护作用。BIX02189(10 μM)抑制ERK5磷酸化,并降低由异丙肾上腺素刺激的新生大鼠心肌细胞(NRCMs)中的肌细胞增强因子2(MEF2)转录活性。 |
激酶实验 | Catalytic assay: MEK5 protein isolated from the baculovirus expression system is used to measure kinase activity utilizing PKLight ATP Detection Reagent. The assay is performed using 15 nM GST-MEK5 and 0.75 μM ATP in assay buffer consisting of 25 mM Hepes, pH 7.5, 10 mM MgCl2, 50 mM KCl, 0.2% BSA, 0.01% CHAPS, 100 μM Na3VO4, 0.5 mM DTT and 1% DMSO in the presence of varying concentrations of BIX02189. The kinase reaction mixture is incubated for 90 minutes at room temperature followed by addition of 10 μL of ATP detection reagent for 15 minutes. The relative light unit (RLU) signal is measured and the RLU signals are converted to percent of control (POC) values for the determination of IC50 value. |
细胞实验 | The cells are serum starved for 20 hours prior to stimulation with sorbitol at a final concentration of 0.4 M for 20 minutes at 37 °C. BIX02189 is added 1.5 hours prior to the addition of sorbitol. The cells are harvested and lysed in 50 μL RIPA buffer containing Halt protease and phosphate inhibitors at 4 °C for 5-10 minutes. The lysates are centrifuged for 10 minutes at 14,000 rpm and 50 μL lysate is added to 50 μl 2× sample buffer and boiled for 4 minutes at 95 °C. Twenty microliters sample is run on SDS–PAGE 10% Tris-glycine gels and transferred to nitrocellulose. Western blotting is done with appropriate antibodies. (Only for Reference) |
分子量 | 440.54 |
分子式 | C27H28N4O2 |
CAS No. | 1094614-85-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 50 mg/mL (113.5 mM), Sonication is recommended.
Ethanol: 74 mg/mL (168 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.2699 mL | 11.3497 mL | 22.6994 mL | 56.7485 mL |
5 mM | 0.454 mL | 2.2699 mL | 4.5399 mL | 11.3497 mL | |
10 mM | 0.227 mL | 1.135 mL | 2.2699 mL | 5.6749 mL | |
20 mM | 0.1135 mL | 0.5675 mL | 1.135 mL | 2.8374 mL | |
50 mM | 0.0454 mL | 0.227 mL | 0.454 mL | 1.135 mL | |
100 mM | 0.0227 mL | 0.1135 mL | 0.227 mL | 0.5675 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。
BIX02189 1094614-85-3 MAPK Stem Cells ERK MEK TGF-beta/Smad BIX-02189 BIX 02189 Inhibitor inhibitor inhibit