购物车
- 全部删除
- 您的购物车当前为空
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。
为众多的药物研发团队赋能,
让新药发现更简单!
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 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 220 | 现货 | |
5 mg | ¥ 478 | 现货 | |
10 mg | ¥ 732 | 现货 | |
25 mg | ¥ 1,180 | 现货 | |
50 mg | ¥ 2,210 | 现货 | |
100 mg | ¥ 3,190 | 现货 | |
200 mg | ¥ 4,490 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 548 | 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 | 在用INH14处理的细胞中,TLR2通路部分蛋白质的过表达显示目标位于复合体TAK1/TAB1下游。INH14减少了由脂肽(TLR2配体)激活的细胞中IkBα的降解。通过激酶实验确认,INH14的靶点是激酶IKKα和/或IKKβ(IC50 IKKα=8.97μM; IC50 IKKβ=3.59μM)。 |
体内活性 | 体内实验显示,INH14减少了脂肽诱导炎症后形成的TNFα,治疗卵巢癌细胞时,INH14降低了NF-kB的固有活性,并减少了这些细胞的伤口愈合能力。 |
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 |
Smiles | CCc1ccc(NC(=O)Nc2ccccc2)cc1 |
密度 | 1.185 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 100 mg/mL (416.14 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
|
版权所有©2015-2024 TargetMol Chemicals Inc.保留所有权利.
评论内容