Biological Activity
Potent and selective IKKβ inhibitor (IC50 = 37 nM). Displays selectivity over 85 other kinases. Inhibits IL-1β-induced TNF-α production in a steroid-insensitive in vitro model of oxidative stress.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Technical Data
| M. Wt | 619.09 |
| Formula | C32H32ClFN6O4 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1187460-81-6 |
| PubChem ID | 57519531 |
| InChI Key | JUOWWGNRWRLBSV-MEKGRNQZSA-N |
| Smiles | FC(C=C4)=CC=C4N(N=C3C(N)=O)C2=C3CCC1=CC=C(NC(C5=CC(N(C6)C[C@@](C)(CO)[C@]6(CO)C)=NC=C5Cl)=O)C=C12 |
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.
Preparing Stock Solutions
The following data is based on the product molecular weight 619.09. 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 |
|---|---|---|---|
| 1 mM | 1.62 mL | 8.08 mL | 16.15 mL |
| 5 mM | 0.32 mL | 1.62 mL | 3.23 mL |
| 10 mM | 0.16 mL | 0.81 mL | 1.62 mL |
| 50 mM | 0.03 mL | 0.16 mL | 0.32 mL |
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References
References are publications that support the products' biological activity.
Sommers et al (2009) Novel tight-binding inhibitory factor-κB kinase (IKK-2) inhibitors demostrate target-specific anti-inflammatory activities in cellular assays and following oral and local delivery in an in vivo model of airway inflammation. J.Pharmacol.Exp.Ther. 330 377 PMID: 19478133
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