Catalog Number: 2539
Chemical Name: N-(4-Pyrrolidin-1-yl-piperidin-1-yl)-[4-(4-benzo[b]thiophen-2-yl-pyrimidin-2-ylamino)phenyl]carboxamide hydrochloride
Biological Activity
Selective inhibitor of IκB kinase (IKK) (IC50 values are 40, 70 and 200 nM for IKKβ, IKK complex and IKKα respectively). Inhibits TNF-α-stimulated IκB degradation and expression of adhesion molecules E-selectin, ICAM and VCAM (IC50 values are 1.0, 0.5, 0.3 and 0.3 μM respectively). Inhibits LPS-induced TNF-α release in vivo and neutrophil extravasion in thioglycollate-induced peritonitis.
Technical Data
  • M.Wt:
    520.09
  • Formula:
    C28H29N5OS.HCl
  • Solubility:
    Soluble to 50 mM in water and to 50 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Desiccate at -20°C
  • CAS No:
    1186195-62-9
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.
Background References
  1. Design and preparation of 2-benzoamido-pyrimidines as inhibitors of IKK.
    Waelchli et al.
    Bioorg.Med.Chem.Lett., 2006;16:108
Citations:

The citations listed below are publications that use Tocris products. Selected citations for IKK 16 include:

3 Citations: Showing 1 - 3
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  1. Inhibition of IκB Kinase Attenuates the Organ Injury and Dysfunction Associated with Hemorrhagic Shock.
    Authors: Sordi Et al.
    J Neuroimmunol 2015;21:563
  2. IKK regulates the deubiquitinase CYLD at the postsynaptic density.
    Authors: Thein Et al.
    Biochem Biophys Res Commun 2014;450:550
  3. Norepinephrine potentiates proinflammatory responses of human vaginal epithelial cells.
    Authors: Brosnahan Et al.
    Bioorg Med Chem Lett 2013;259:42583

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