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INH14

Catalog No. T5209 CAS 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).

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INH14, CAS 200134-22-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 38.00
2 mg	In stock	$ 54.00
5 mg	In stock	$ 85.00
10 mg	In stock	$ 126.00
25 mg	In stock	$ 207.00
50 mg	In stock	$ 369.00
100 mg	In stock	$ 549.00
1 mL * 10 mM (in DMSO)	In stock	$ 88.00

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Purity: 95.41%

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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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (416.14 mM)

References and Literature

1. Drexel M, et al. INH14, a Small-Molecule Urea Derivative, Inhibits the IKKα/β-Dependent TLR Inflammatory Response. Chembiochem. 2019 Mar 1;20(5):710-717.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Active Compound Library NF-κB Signaling Compound Library Kinase Inhibitor Library Anti-Breast Cancer Compound Library Anti-Prostate Cancer Compound Library HIF-1 Signaling Pathway Compound Library Immunology/Inflammation Compound Library Anti-Ovarian Cancer Compound Library Target-Focused Phenotypic Screening Library

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Keywords

INH14 200134-22-1 NF-Κb IκB/IKK inhibit IKK IκB kinase INH 14 I kappa B kinase INH-14 Inhibitor inhibitor

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