IKK-2 Inhibitor VIII

Biochem/physiol Actions

Target IC₅₀: 8.5 and 250 nM for IKK-2 and IKK-1, respectively

Reversible: no

Product does not compete with ATP.

Primary TargetIKK-2

Cell permeable: yes

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.

Legal Information

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

Other Notes

Murata, T., et al. 2004. Bioorg. Med. Chem. Lett.14, 4019.

Packaging

1 mg in Plastic ampoule

Packaged under inert gas

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.

Warning

Toxicity: Irritant (B)