Product Details
Product Name:
INH14 |
CAS No.:
200134-22-1 |
Purity:
95.41% |
Supply Ability:
10g |
Release date:
2024/11/17 |
Product Introduction
Bioactivity
名稱 | INH14 |
描述 | INH14 is a novel inhibitor of the IKKα/β-dependent TLR inflammatory response (IC50s: 8.97/3.59 μM for IKKα/IKKβ). |
細(xì)胞實(shí)驗(yàn) | 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. |
激酶實(shí)驗(yàn) | 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. |
動(dòng)物實(shí)驗(yàn) | 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. |
體外活性 | 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). |
體內(nèi)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. |
存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 100 mg/mL (416.14 mM)
|
關(guān)鍵字 | inhibit | IKK | IκB kinase | INH 14 | I kappa B kinase | INH-14 | INH14 | Inhibitor |
相關(guān)產(chǎn)品 | JTP 0819958 - HOIPIN-1 | WS3 | Amlexanox | Malachite green oxalate | BAY 11-7082 | SC-514 | Resveratrol | Bardoxolone Methyl | Bay 11-7085 | GSK8612 | BX795 | Allicin |
相關(guān)庫(kù) | 經(jīng)典已知活性庫(kù) | 抗抑郁癥化合物庫(kù) | 激酶抑制劑庫(kù) | 抑制劑庫(kù) | NO PAINS 化合物庫(kù) | 抗前列腺癌化合物庫(kù) | 抗衰老化合物庫(kù) | 已知活性化合物庫(kù) | 抗癌化合物庫(kù) | 抗癌活性化合物庫(kù) |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
Product name |
Price |
|
Suppliers |
Update time |
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$/ |
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Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |