IKK-2 Inhibitor V

Biochem/physiol Actions

Reversible: no

Product does not compete with ATP.

Primary TargetIKK-2

Target IC₅₀: ~ 250 nM blocking IκBα phosphorylation

Cell permeable: yes

General description

A cell-permeable IKK-2 inhibitor that selectively blocks IκBα phosphorylation (IC₅₀ ~250 nM) and prevents the induction of NF-κB p65 nuclear translocation. Reported to suppress neoplastic proliferation of mast cells with constitutively activated c-kit receptor. Shown to offer cardioprotection by reducing IL-1β and MCP-1 production (IC₅₀﹤1 µM) in cardiomyocytes, and ameliorate insulin resistance in diabetic KKA_y mice by regulating adiponectin release.

A cell-permeable salicylamide compound that acts as an IKK-2 inhibitor by selectively blocking IκBα phosphorylation (IC₅₀ ~ 250 nM) and thereby prevents the induction of NF-κB p65 nuclear translocation. Shown to offer cardioprotection by reducing IL-1β and MCP-1 production (IC₅₀﹤1 µM) in cardiomyocytes, and ameliorate insulin resistance in KKA_y mice by regulating adiponectin release.

Legal Information

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

Other Notes

Kamon, J., et al. 2004. Biochem. Biophys. Res. Commun.323, 242.Onai, Y., et al. 2004. Cardiovasc. Res.63, 51.Tanaka, A., et al. 2004. Blood105, 2324.

Packaging

Packaged under inert gas

5 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)