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Submit ReviewIKK 16
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)
Biological Activity for IKK 16
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.
Compound Libraries for IKK 16
IKK 16 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.
Technical Data for IKK 16
| 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 for IKK 16
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 26 | 50 | |
| DMSO | 26 | 50 |
Preparing Stock Solutions for IKK 16
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 |
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Product Datasheets for IKK 16
References for IKK 16
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.
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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
8 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
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
Shen et al (2013) Small-molecule inducer of β cell proliferation identified by high-throughput screening. J.Am.Chem.Soc. 135 1669 PMID: 23330637
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
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
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) NE 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? Please let us know.
Reviews for IKK 16
Average Rating: 5 (Based on 1 Review.)
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IKK 16 blocks LPA-mediated COX-2 expression.
By
Anonymous on 12/13/2018
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: Osteosarcoma
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
