SC 514

Catalog # Availability Size / Price Qty
3318/10
3318/50
SC 514 | CAS No. 354812-17-2 | IkB Kinase Inhibitors
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Description: IKKβ inhibitor; attenuates NF-κB-induced gene expression

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

Purity: ≥98%

Product Details
Citations (3)
Reviews (1)

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.

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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold for research purposes under agreement from AstraZeneca

Background References

  1. 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
  2. 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
  3. Hit-to-lead studies: the discovery of potent, orally active thiophenecarboxamide IKK-2 inhibitors.
    Baxter et al.
    Bioorg.Med.Chem.Letts., 2004;14:2817

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Citations for SC 514

The citations listed below are publications that use Tocris products. Selected citations for SC 514 include:

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SC 514 inhibits LPS-mediated inflammation
By Anonymous on 12/11/2018
Species: Mouse

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.


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