Description General description A cell-permeable piperidinyl-pyridine compound that acts as a selective inhibitor of IKK-2 activity (IC50 = 8.5 and 250 nM for IKK-2 and IKK-1, respectively) with little effect towards IKK-3, Syk, and MKK4 (IC50 >20 µM). Exhibits good aqueous solubility (0.12 mg/ml in pH 7.4 isotonic buffer) and potent activity in various cellular assays in vitro (IC50<150 nM). Shown to be orally bioavailable both in rats and mice (BA = 60% and 16%, respectively) and effectively inhibit arachidonic acid-induced swelling in a murine ear edema model in vivo. Packaging 1 mg in Plastic ampoule Biochem/physiol Actions Cell permeable: yes Primary Target IKK-2 Product does not compete with ATP. Reversible: no Target IC50: 8.5 and 250 nM for IKK-2 and IKK-1, respectively Packaging Packaged under inert gas Warning Toxicity: Irritant (B) Preparation Note Sonication is required for complete solubilization. Reconstitution Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. Other Notes Murata, T., et al. 2004. Bioorg. Med. Chem. Lett.14, 4019.