Biochem/physiol Actions

Reversible: yes

Product competes with ATP.

Primary TargetIKK-2

Cell permeable: yes

Target IC₅₀: 3-12 µM for IKK-2 homodimer, IKK-1/IKK-2 heterodimer, and IKK-2

General description

A cell-permeable (thienothienyl)amino-acetamide compound that displays anti-inflammatory properties. Acts as a potent, reversible, ATP-competitive, and highly selective inhibitor of IKK-2 (IC₅₀ = ~ 3-12 µM for IKK-2 homodimer, IKK-1/IKK-2 heterodimer, and IKK-2). Its specificity has been confirmed using a panel of 31 other kinases, including IKK isoforms IKK-1, IKK-i, and TBK-1 (IC₅₀ >200 µM). Shown to specifically block NF-κB-dependent gene expression, but not MAP kinase pathways, in stimulated synovial fibroblasts RASF. A 25 mM (1 mg/178 µl) solution of IKK-2 Inhibitor, SC-514 (Cat. No. 401485) in DMSO is also available.

A cell-permeable, potent, reversible, ATP-competitive and highly selective inhibitor of IKK-2 (IC₅₀ ~3-12 µM for IKK-2 homodimer, IKK-1/IKK-2 heterodimer, and IKK-2) that also displays anti-inflammatory properties. Specificity has been reported using a panel of 31 additional kinases, including IKK isoforms IKK-1, IKK-i, and TBK-1 (IC₅₀ >200 µM). Shown to specifically block NF-κB-dependent gene expression, but not MAP kinase pathways, in stimulated RASF synovial fibroblast cells. Does not inhibit the phosphorylation and activation of the IKK complex.

Legal Information

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

Other Notes

Baxter, A., et al. 2004 Bioorg. Med. Chem. Lett.14, 2817.Kishore, N., et al. 2003. J. Biol. Chem.278, 32861.

Packaging

1 mg in Plastic ampoule

Packaged under inert gas

Reconstitution

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

Warning

Toxicity: Carcinogenic / Teratogenic (D)