Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PS-1145 (IKK Inhibitor X) 是一种 IκB 激酶抑制剂,IC50为 88 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 292 | 现货 | ||
2 mg | ¥ 413 | 现货 | ||
5 mg | ¥ 713 | 现货 | ||
10 mg | ¥ 1,230 | 现货 | ||
25 mg | ¥ 2,390 | 现货 | ||
50 mg | ¥ 3,620 | 现货 | ||
100 mg | ¥ 5,220 | 现货 | ||
500 mg | ¥ 10,900 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 743 | 现货 |
产品描述 | PS-1145 (IKK Inhibitor X) is a specific IKK inhibitor with IC50 of 88 nM. |
靶点活性 | IKKϵ:88 nM |
体外活性 | 50 mg/kg PS-1145 (i.v.)通过上调患有DMBA诱发的皮肤肿瘤的雄性Wistar大鼠中p53,激活胱天蛋白酶,并下调NF-κB和VEGF因子,增强肿瘤细胞凋亡. |
体内活性 | PS-1145抑制人初级CD4(+) T细胞增殖,并通过CD3和CD28共同受体的参与阻碍响NF-κB 和 AP-1转录因子的活化。PS-1145通过抑制IkappaBalpha磷酸化阻断TNFalpha-诱导的NF-kappaB活化,并阻断IL-6对Dex-诱导的细胞凋亡的保护作用。 |
激酶实验 | Kinase assay: PS-1145 are dissolved in DMSO and stored at ?20?°C until use. Ki value of PS-1145 against the IKK complex is determined by measuring Km ,?ATP against varying fixed concentration of the inhibitor. Briefly, partially purified IKK complex obtained from unstimulated HeLa S3 cells are pre-activated using the catalytic domain of MEKK1 expressed in sf9. Kinase activity is assessed using a biotinylated IκBα peptide (250 μM, RHDSGLDSMKD,Km ,peptide = 30 μM,K m ,?ATP = 10 μM) and phospho-[Ser32]-phosphoantibodies in an ELISA format with appropriate standard curve for quantification. For PS-1145 Ki measurement, the activated IKK complex is first preincubated in varying fixed concentration of the inhibitor (0.1–1 μM) at 25 °C for 1 h. Then apparentK m measurement for MgATP is performed at each discrete inhibitor concentration. |
细胞实验 | The inhibitory effect of PS-1145 on MM growth is assessed by measuring MTT dye absorbance of the cells. Cells from 48-h cultures are pulsed with 10 μL of 5 mg/ml MTT to each well for the last 4 h of 48-h cultures, followed by 100 μl of isopropanol containing 0.04N HCl. Absorbance is measured at 570 nm using a spectrophotometer. (Only for Reference) |
别名 | IKK Inhibitor X |
分子量 | 322.75 |
分子式 | C17H11ClN4O |
CAS No. | 431898-65-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 60 mg/mL (185.9 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 2 mg/mL(6.19 mM), Heating is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 3.0984 mL | 15.4919 mL | 30.9837 mL | 77.4593 mL |
5 mM | 0.6197 mL | 3.0984 mL | 6.1967 mL | 15.4919 mL | |
DMSO | 10 mM | 0.3098 mL | 1.5492 mL | 3.0984 mL | 7.7459 mL |
20 mM | 0.1549 mL | 0.7746 mL | 1.5492 mL | 3.873 mL | |
50 mM | 0.062 mL | 0.3098 mL | 0.6197 mL | 1.5492 mL | |
100 mM | 0.031 mL | 0.1549 mL | 0.3098 mL | 0.7746 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。
PS-1145 431898-65-6 Apoptosis NF-Κb IκB/IKK I kappa B kinase PS1145 inhibit IKK PS 1145 IKK Inhibitor X IκB kinase Inhibitor inhibitor