R&D Systems Inc. Tocris Bioscience Boston Biochem

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.

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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