Selective allosteric inhibitor of IKK (IC50
values are 0.3 and 4.0 μ
M for IKKβ
respectively). Exhibits no effect against a panel of 15 other kinases. Attenuates LPS-induced cytokine production in vitro
and blocks NFκ
B dependent transcription in mice. Also suppresses joint destruction in a mouse model of arthritis.
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All Tocris products are intended for laboratory research use only.
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.
Burke et al.
Inhibition of choriodecidual cytokine production and inflammatory gene expression by selective IκB kinase (IKK) inhibitors.
De Silva et al.
Collagen and aggrecan degradation is blocked in interleukin-1-treated cartilage explants by an inhibitor of IκB kinase through suppression of metalloproteinase expression.
Pattoli et al.