Catalog Number: 3318
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.
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.
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
Citations:

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

1 Citations: Showing 1 - 1

  1. 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

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