Powder: -20°C for 3 years | In solvent: -80°C for 1 year
INH14 是 IKKα (IC50:8.97 μM) / IKKβ (IC50:3.59 μM) 的抑制剂。它能够抑制 IKKα/β 依赖性 TLR 炎症反应,抑制 TAK1/TAB1 的下游和 NF-kB 信号通路。它具有抗炎和抗癌作用。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 367 | 现货 | ||
2 mg | ¥ 526 | 现货 | ||
5 mg | ¥ 797 | 现货 | ||
10 mg | ¥ 1,220 | 现货 | ||
25 mg | ¥ 1,980 | 现货 | ||
50 mg | ¥ 3,690 | 现货 | ||
100 mg | ¥ 5,320 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 913 | 现货 |
产品描述 | INH14 is a novel inhibitor of the IKKα/β-dependent TLR inflammatory response (IC50s: 8.97/3.59 μM for IKKα/IKKβ). |
靶点活性 | IKKβ:3.59 μM (cell free), IKKα:8.97 μM (cell free) |
体外活性 | Overexpression of proteins that are part of the TLR2 pathway in cells treated with INH14 indicated that the target lay downstream of the complex TAK1/TAB1. INH14 decreased IkBα degradation in cells activated by lipopeptide (TLR2 ligand). The kinases IKKα and/or IKKβ were the targets of INH14, which was confirmed with kinase assays (IC50 IKKα=8.97?μM; IC50 IKKβ=3.59?μM). |
体内活性 | In vivo experiments showed that INH14 decreased TNFα formed after lipopeptide-induced inflammation, and treatment of ovarian cancer cells with INH14 led to a reduction of NF-kB constitutive activity and a reduction in the wound-closing ability of these cells. |
激酶实验 | IKKα and IKKβ kinase assays (ADP-GloTM 109 kinase assay) were purchased from Promega and used following the manufacturer′s instructions. The quantification of the ADP produced in the reactions (chemiluminescence) was measured with a Victor plate reader. IKKα (15 ng per reaction) or IKKβ (20 ng per reaction) were incubated with ATP (50 μM or 25 μM, respectively) and substrate-peptide (0.2 ng/ml) in the presence of vehicle or increasing concentrations of INH14 at room temperature for one hour. |
细胞实验 | Human primary monocytes (8 x 10^4 cells/well) were seeded and incubated overnight with the compound, media control, or SDS (0.02%). Then, the tetrazolium salt WST-8 was added, and the cells were incubated for one additional hour at 37°C. During this period, the dehydrogenase activity of viable cells led to the production of the coloured product (formazan). The cell viability was measured with a Victor plate reader as an increase in the absorbance at 450 nm. |
动物实验 | 8-week old, male, pathogen-free C57BL/6J mice were maintained at the animal facility (12 h light/dark cycle; standard rodent chow and water available ad libitum). For lipopeptide-induced inflammation, 5 μg/g of INH14 or vehicle were administered intraperitoneally. After one hour, P2 (2.5 μg/g) was injected and 25 μl of tail vein blood were collected at that time point (0 h) and 2 h after. The blood was centrifuged at 5 x 10^3 x g, and the supernatant frozen at -20 °C until further cytokine measurement by ELISA. |
分子量 | 240.3 |
分子式 | C15H16N2O |
CAS No. | 200134-22-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (416.14 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 4.1615 mL | 20.8073 mL | 41.6146 mL | 104.0366 mL |
5 mM | 0.8323 mL | 4.1615 mL | 8.3229 mL | 20.8073 mL | |
10 mM | 0.4161 mL | 2.0807 mL | 4.1615 mL | 10.4037 mL | |
20 mM | 0.2081 mL | 1.0404 mL | 2.0807 mL | 5.2018 mL | |
50 mM | 0.0832 mL | 0.4161 mL | 0.8323 mL | 2.0807 mL | |
100 mM | 0.0416 mL | 0.2081 mL | 0.4161 mL | 1.0404 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。
INH14 200134-22-1 NF-Κb IκB/IKK inhibit IKK IκB kinase INH 14 I kappa B kinase INH-14 Inhibitor inhibitor