INH14

SKU: orb1301996

Description

INH14 is a novel small molecule inhibitor that selectively targets IKKα and IKKβ with IC50 values of 8.97 μM and 3.59 μM, respectively. It is a valuable research tool for studying the IKK-dependent TLR inflammatory signaling pathway in both cellular and animal models of inflammation and immune response.

Research Area

Signal Transduction

Key Properties

• CAS Number: 200134-22-1
• MW: 240.3
• Purity: 96.66% (May vary between batches)
• Formula: C₁₅H₁₆N₂O
• SMILES: CCc1ccc(NC(=O)Nc2ccccc2)cc1
• Target: IκB/IKK
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (16.65 mM);DMSO:100 mg/mL (416.15 mM)

Bioactivity

• Target IC50:
  IKKβ:3.59 μM (cell free)|IKKα:8.97 μM (cell free)
• 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.
  Read more...
• 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).
  Read more...
• 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.
  Read more...
• 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.
  Read more...

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

I kappa B kinase, Inhibitor, IkB, IkB/IKK, IKK, INH14, INH-14, INH 14, inhibit, IκB, IκB kinase, IKKα, IKKβ

Compound Identifiers

PubChem CID

295048