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INH14
🥰Excellent
Catalog No. T5209Cas No. 200134-22-1
INH14 is a novel inhibitor of the IKKα/β-dependent TLR inflammatory response (IC50s: 8.97/3.59 μM for IKKα/IKKβ).
INH14
🥰Excellent
Purity: 95.41%
Catalog No. T5209Cas No. 200134-22-1
INH14 is a novel inhibitor of the IKKα/β-dependent TLR inflammatory response (IC50s: 8.97/3.59 μM for IKKα/IKKβ).
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 2 mg | $32 | In Stock | |
| 5 mg | $51 | In Stock | |
| 10 mg | $76 | In Stock | |
| 25 mg | $123 | In Stock | |
| 50 mg | $221 | In Stock | |
| 100 mg | $329 | In Stock | |
| 200 mg | $475 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $53 | In Stock |
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Purity:95.41%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | INH14 is a novel inhibitor of the IKKα/β-dependent TLR inflammatory response (IC50s: 8.97/3.59 μM for IKKα/IKKβ). |
| Targets&IC50 | IKKβ:3.59 μM (cell free), IKKα:8.97 μM (cell free) |
| In vitro | 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). |
| In vivo | 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. |
| Kinase Assay | 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. |
| Cell Research | 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. |
| Animal Research | 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. |
| Molecular Weight | 240.3 |
| Formula | C15H16N2O |
| Cas No. | 200134-22-1 |
| Smiles | CCc1ccc(NC(=O)Nc2ccccc2)cc1 |
| Relative Density. | 1.185 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 100 mg/mL (416.14 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
Dose Conversion
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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