Cat. No. 3318
Chemical Name: 4-Amino-[2',3'-bithiophene]-5-carboxa
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.
Licensing InformationSold for research purposes under agreement from AstraZeneca
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.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Gomez et al (2005) Selective inhibition of kappa B kinase-β aborgates induction of nitric oxide synthase in lipopolysaccharide-stimulated rat aortic smooth muscle cells. Br.J.Pharmacol. 146 217. PMID: 15997236.
Baxter et al (2004) Hit-to-lead studies: the discovery of potent, orally active thiophenecarboxamide IKK-2 inhibitors. Bioorg.Med.Chem.Letts. 14 2817.
Kishore et al (2003) A selective IKK-2 inhibitor blocks NF-κB-dependent gene expression in interleukin-1β-stimulated synovial fibroblasts. J.Biol.Chem. 278 32861. PMID: 12813046.
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Citations are publications that use Tocris products. Selected citations for SC 514 include:
Akhtar et al (2015) MicroRNA-602 and microRNA-608 regulate sonic hedgehog expression via target sites in the coding region in human chondrocytes. Nature 67 423. PMID: 25385442.
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Keywords: SC 514, supplier, IKK-2, inhibitors, inhibits, attenuates, NF-κB, NF-kappaB-induced, gene, expression, NF-kB, IKK, IκB, IkappaB, Kinases, Nuclear, Factor, Kappa, B, NF-kappaB, Cytokine, Signaling, Signalling, Transcription, Factors, SC514, AstraZeneca, Tocris Bioscience, IκB Kinase Inhibitor products
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