IKK 16
Chemical Name: N-(4-Pyrrolidin-1-yl-piperidin-1-yl)-[4-(4-benzo[b]thiophen-2-yl-pyrimidin-2-ylamino)phenyl]carboxamide hydrochloride
Purity: ≥98%
Biological Activity
IKK 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.Technical Data
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.
Background References
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Design and preparation of 2-benzoamido-pyrimidines as inhibitors of IKK.
Waelchli et al.
Bioorg.Med.Chem.Lett., 2006;16:108
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Citations for IKK 16
The citations listed below are publications that use Tocris products. Selected citations for IKK 16 include:
8 Citations: Showing 1 - 8
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Profiling drugs for rheumatoid arthritis that inhibit synovial fibroblast activation.
Authors: Jones Et al.
Nat Chem Biol 2017;13:38
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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.
Oncotarget 2016;7:14220
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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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Inhibition of IκB Kinase Attenuates the Organ Injury and Dysfunction Associated with Hemorrhagic Shock.
Authors: Sordi Et al.
J Neuroimmunol 2015;21:563
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IKK regulates the deubiquitinase CYLD at the postsynaptic density.
Authors: Thein Et al.
Biochem Biophys Res Commun 2014;450:550
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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
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NE potentiates proinflammatory responses of human vaginal epithelial cells.
Authors: Brosnahan Et al.
Bioorg Med Chem Lett 2013;259:42583
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Small-molecule inducer of β cell proliferation identified by high-throughput screening.
Authors: Shen Et al.
J.Am.Chem.Soc. 2013;135:1669
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