SC 514

Cat. No. 3318

SC 514 C9H8N2OS2 [354812-17-2]

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Chemical Name: 4-Amino-[2',3'-bithiophene]-5-carboxamide

Biological Activity

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.

Licensing Information

Sold for research purposes under agreement from AstraZeneca

Technical Data

M.Wt:
224.3
Formula:
C9H8N2OS2
Solubility:
Soluble to 100 mM in DMSO and to 10 mM in ethanol
Purity:
>98 %
Storage:
Store at +4°C
CAS No:
354812-17-2

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 / Safety Data Sheet

Certificate of Analysis: View current batch
Safety Data Sheet: View Safety Data Sheet

References

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.

Baxter et al (2004) Hit-to-lead studies: the discovery of potent, orally active thiophenecarboxamide IKK-2 inhibitors. Bioorg.Med.Chem.Letts. 14 2817.

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.

If you know of a relevant citation for this product please let us know.

Keywords: SC 514, supplier, IKK-2, inhibitors, 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

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