SC 514
Chemical Name: 4-Amino-[2',3'-bithiophene]-5-carboxamide
Purity: ≥98%
Biological Activity
SC 514 is an orally 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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
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A selective IKK-2 inhibitor blocks NF-κB-dependent gene expression in interleukin-1β-stimulated synovial fibroblasts.
Kishore et al.
J.Biol.Chem., 2003;278:32861 -
Selective inhibition of kappa B kinase-β aborgates induction of nitric oxide synthase in lipopolysaccharide-stimulated rat aortic smooth muscle cells.
Gomez et al.
Br.J.Pharmacol., 2005;146:217 -
Hit-to-lead studies: the discovery of potent, orally active thiophenecarboxamide IKK-2 inhibitors.
Baxter et al.
Bioorg.Med.Chem.Letts., 2004;14:2817
Product Datasheets
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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
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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
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MicroRNA-602 and microRNA-608 regulate sonic hedgehog expression via target sites in the coding region in human chondrocytes.
Authors: Akhtar Et al.
Nature 2015;67:423
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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.
Virology 2015;485:340
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