Selective 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.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 291.78. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||3.43 mL||17.14 mL||34.27 mL|
|5 mM||0.69 mL||3.43 mL||6.85 mL|
|10 mM||0.34 mL||1.71 mL||3.43 mL|
|50 mM||0.07 mL||0.34 mL||0.69 mL|
References are publications that support the biological activity of the product.
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
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
If you know of a relevant reference for BMS 345541, please let us know.
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