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 (3)
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.92 mL 9.61 mL 19.23 mL
5 mM 0.38 mL 1.92 mL 3.85 mL
10 mM 0.19 mL 0.96 mL 1.92 mL
50 mM 0.04 mL 0.19 mL 0.38 mL

Molarity Calculator

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Reconstitution Calculator

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

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


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View all IκB Kinase Inhibitors

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, IkB, Kinase, Tocris Bioscience

3 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

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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Pathways for IKK 16

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