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SC 514

Catalog #: 3318
3 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
3318/10
3318/50
SC 514 | CAS No. 354812-17-2 | IkB Kinase Inhibitors
1 Image
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
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

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

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 key role for the endothelium in NOD1 mediated vascular inflammation: comparison to TLR4 responses.
    Gatheral T, Reed D, Moreno L, Gough P, Votta B, Sehon C, Rickard D, Bertin J, Lim E, Nicholson A, Mitchell J
    PLoS ONE, 2012;7(8):e42386.
  2. Trail (TNF-related apoptosis-inducing ligand) induces an inflammatory response in human adipocytes
    V Zoller, JB Funcke, J Roos, M Dahlhaus, M Abd El Hay, K Holzmann, R Marienfeld, T Kietzmann, KM Debatin, M Wabitsch, P Fischer-Po
    Sci Rep, 2017;7(1):5691.
  3. 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
  4. 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
  5. 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

  1. 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
  2. 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
  3. 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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