General description

A cell-permeable amino-diarylbenzamide compound that acts as a potent ATP site-targeting inhibitor against IKK-1 and IKK-2 (pIC₅₀ = 6.4 and 7.0, respectively), while exhibiting more than 50-fold less potency toward a panel of greater than 50 other kinases, including IKK-3 (pIC₅₀﹤4.8), ALK5, Cdk-2, EGFR, ErbB2, GSK-3β, Plk1, Src, and VEGFR-2. Shown to effectively suppress LPS-stimulated secretion of TNF-α, IL-1β, and IL-6 from human PBMCs (pIC₅₀ = 6.1, 6.4, and 5.7, respectively) as well as TNF-α-induced NF-κB nuclear translocation in human lung fibroblast cells (pIC₅₀ = 5.7).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Christopher, J.A., et al. 2007. Bioorg. Med. Chem. Lett.17, 3972.

Packaging

5 mg in Glass bottle

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)