Orally active, ATP-competitive IKKβ
= 3 - 12 μ
M) that displays > 10-fold selectivity over 28 other kinases including JNK, p38, MK2 and ERK. Attenuates NF-κ
B-induced gene expression of IL-6, IL-8 and COX-2 in synovial fibroblasts (IC50
values are 20, 20 and 8 μ
M respectively). Reduces iNOS induction and exhibits anti-inflammatory activity in vivo
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A selective IKK-2 inhibitor blocks NF-κB-dependent gene expression in interleukin-1β-stimulated synovial fibroblasts.
Kishore et al.
Selective inhibition of kappa B kinase-β aborgates induction of nitric oxide synthase in lipopolysaccharide-stimulated rat aortic smooth muscle cells.
Gomez et al.
Hit-to-lead studies: the discovery of potent, orally active thiophenecarboxamide IKK-2 inhibitors.
Baxter et al.
The citations listed below are publications that use Tocris products. Selected citations for SC 514 include:
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