IKK 16

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Cat.No. 2539 - IKK 16 | C28H29N5OS.HCl | CAS No. 1186195-62-9
Description: Selective inhibitor of IKK
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% (HPLC)
Datasheet
Citations (7)
Reviews
Literature

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.

Compound Libraries

IKK 16 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 520.09
Formula C28H29N5OS.HCl
Storage Desiccate at -20°C
Purity ≥98% (HPLC)
CAS Number 1186195-62-9
PubChem ID 56972179
InChI Key XFVDIVQCZWDBCW-UHFFFAOYSA-N
Smiles Cl.O=C(N1CCC(CC1)N1CCCC1)C1=CC=C(NC2=NC=CC(=N2)C2=CC3=CC=CC=C3S2)C=C1

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 26 50
DMSO 26 50

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 solvent 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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

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


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

View Related Products by Product Action

View all IκB Kinase Inhibitors

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:

Jones et al (2017) Profiling drugs for rheumatoid arthritis that inhibit synovial fibroblast activation. Nat Chem Biol 13 38 PMID: 27820799

Brosnahan et al (2013) Norepinephrine potentiates proinflammatory responses of human vaginal epithelial cells. Bioorg Med Chem Lett 259 42583 PMID: 23571017

Thein et al (2014) IKK regulates the deubiquitinase CYLD at the postsynaptic density. Biochem Biophys Res Commun 450 550 PMID: 24928390

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

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


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