Cat. No. 4806
Chemical Name: N1-(1,8-Dimethylimidazo[1,2-a]quino
Biological ActivitySelective allosteric inhibitor of IKK (IC50 values are 0.3 and 4.0 μM for IKKβ and IKKα respectively). Exhibits no effect against a panel of 15 other kinases. Attenuates LPS-induced cytokine production in vitro and blocks NFκB dependent transcription in mice. Also suppresses joint destruction in a mouse model of arthritis.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
De Silva et al (2010) Inhibition of choriodecidual cytokine production and inflammatory gene expression by selective IκB kinase (IKK) inhibitors. Br.J.Pharmacol. 160 1808. PMID: 20649582.
Pattoli et al (2005) Collagen and aggrecan degradation is blocked in interleukin-1-treated cartilage explants by an inhibitor of IκB kinase through suppression of metalloproteinase expression. J.Pharmacol.Exp.Ther. 315 382. PMID: 16009742.
Burke et al (2003) BMS-345541 is a highly selective inhibitor of IκB kinase that binds at an allosteric site of the enzyme and blocks NF- κB-dependent transcription in mice. J.Biol.Chem. 278 1450. PMID: 12403772.
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Keywords: BMS 345541, supplier, BMS345541, Selective, IKK, allosteric, inhibitors, inhibits, anti-inflammatory, IKKβ, IKKμ, arthritis, IKK1, IKK2, Tocris Bioscience, IκB Kinase Inhibitor products
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