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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.
|Storage||Desiccate at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 520.09. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.5 mM||3.85 mL||19.23 mL||38.45 mL|
|2.5 mM||0.77 mL||3.85 mL||7.69 mL|
|5 mM||0.38 mL||1.92 mL||3.85 mL|
|25 mM||0.08 mL||0.38 mL||0.77 mL|
References are publications that support the biological activity of the product.
Waelchli et al (2006) Design and preparation of 2-benzoamido-pyrimidines as inhibitors of IKK. Bioorg.Med.Chem.Lett. 16 108 PMID: 16236504
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Keywords: IKK 16, IKK 16 supplier, Selective, inhibitors, inhibits, IKK, IκB, IkappaB, Kinases, NF-κB, NF-kappaB, NF-kB, Transcription, Factors, Nuclear, Factor, Kappa, B, Cytokine, Signaling, Signalling, IKK16, IkB, Kinase, NF-kB/IkB, 2539, Tocris Bioscience
7 Citations for IKK 16
Citations are publications that use Tocris products. Selected citations for IKK 16 include:
Sordi et al (2015) Inhibition of IκB Kinase Attenuates the Organ Injury and Dysfunction Associated with Hemorrhagic Shock. J Neuroimmunol 21 563 PMID: 26101953
Rycaj et al (2016) 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. Oncotarget 7 14220 PMID: 26871947
Jones et al (2017) Profiling drugs for rheumatoid arthritis that inhibit synovial fibroblast activation. Nat Chem Biol 13 38 PMID: 27820799
Cataldi et al (2015) Breaking resistance of pancreatic cancer cells to an attenuated vesicular stomatitis virus through a novel activity of IKK inhibitor TPCA-1. Virology 485 340 PMID: 26331681
Ansbro et al (2013) Screening compounds with a novel high-throughput ABCB1-mediated efflux assay identifies drugs with known therapeutic targets at risk for multidrug resistance interference. PLoS One 8 e60334 PMID: 23593196
Thein et al (2014) IKK regulates the deubiquitinase CYLD at the postsynaptic density. Biochem Biophys Res Commun 450 550 PMID: 24928390
Brosnahan et al (2013) NE potentiates proinflammatory responses of human vaginal epithelial cells. Bioorg Med Chem Lett 259 42583 PMID: 23571017
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Reviews for IKK 16
Average Rating: 5 (Based on 1 Review.)
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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
Literature in this Area
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