IKK 16

Cat. No. 2539

IKK 16 C28H29N5OS.HCl [1186195-62-9]

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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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Waelchli et al (2006) Design and preparation of 2-benzoamido-pyrimidines as inhibitors of IKK. Bioorg.Med.Chem.Lett. 16 108. PMID: 16236504.

If you know of a relevant reference for IKK 16 please let us know.

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.

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) Norepinephrine potentiates proinflammatory responses of human vaginal epithelial cells. Bioorg Med Chem Lett 259 42583. PMID: 23571017.

Do you know of a great paper that uses IKK 16 from Tocris? If so please let us know.

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Keywords: 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, Tocris Bioscience, IκB Kinase Inhibitor products

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