Chemical Name: 4-Amino-[2',3'-bithiophene]-5-carboxamide
Biological ActivityOrally active, ATP-competitive IKKβ inhibitor (IC50 = 3 - 12 μM) that displays > 10-fold selectivity over 28 other kinases including JNK, p38, MK2 and ERK. Attenuates NF-κB-induced gene expression of IL-6, IL-8 and COX-2 in synovial fibroblasts (IC50 values are 20, 20 and 8 μM respectively). Reduces iNOS induction and exhibits anti-inflammatory activity in vivo.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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.
Citations for SC 514
The citations listed below are publications that use Tocris products. Selected citations for SC 514 include:
3 Citations: Showing 1 - 3
Inhibition of Inflammatory Changes in Human Myometrial Cells by Cell Penetrating Peptide and Small Molecule Inhibitors of NFκB.
Authors: Gurney Et al.
Front Immunol 2019;9:2966
MicroRNA-602 and microRNA-608 regulate sonic hedgehog expression via target sites in the coding region in human chondrocytes.
Authors: Akhtar Et al.
Breaking resistance of pancreatic cancer cells to an attenuated vesicular stomatitis virus through a novel activity of IKK inhibitor TPCA-1.
Authors: Cataldi Et al.
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RAW macrophages were incubated with 1 mM SC 514 for 30 min prior to addition of 200 ng/ml LPS for 8 h to follow TNFa mRNA expression. LPS elevated TNFa mRNA levels that was significantly inhibited by pretreatment of cells with SC 514.