Chemical Name: N-(4-Pyrrolidin-1-yl-piperidin-1-yl)-[4-(4-benzo[b]thiophen-2-yl-pyrimidin-2-ylamino)phenyl]carboxamide hydrochloride
Biological ActivityIKK 16 is a 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Design and preparation of 2-benzoamido-pyrimidines as inhibitors of IKK.
Waelchli et al.
Citations for IKK 16
The citations listed below are publications that use Tocris products. Selected citations for IKK 16 include:
7 Citations: Showing 1 - 7
Profiling drugs for rheumatoid arthritis that inhibit synovial fibroblast activation.
Authors: Jones Et al.
Nat Chem Biol 2017;13:38
Longitudinal tracking of subpopulation dynamics and molecular changes during LNCaP cell castration and identification of inhibitors that could target the PSA-/lo castration-resistant cells.
Authors: Rycaj Et al.
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.
Inhibition of IκB Kinase Attenuates the Organ Injury and Dysfunction Associated with Hemorrhagic Shock.
Authors: Sordi Et al.
J Neuroimmunol 2015;21:563
IKK regulates the deubiquitinase CYLD at the postsynaptic density.
Authors: Thein Et al.
Biochem Biophys Res Commun 2014;450:550
Screening compounds with a novel high-throughput ABCB1-mediated efflux assay identifies drugs with known therapeutic targets at risk for multidrug resistance interference.
Authors: Ansbro Et al.
PLoS One 2013;8:e60334
NE potentiates proinflammatory responses of human vaginal epithelial cells.
Authors: Brosnahan Et al.
Bioorg Med Chem Lett 2013;259:42583
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Human osteosarcoma cells were incubated with 5 μM IKK 16 for 30 min prior to treatment with 10 μM LPA to estimate COX-2 expression using Western blot analysis. IKK 16 abolished LPA-induced COX-2 expression