Biological Activity
Selective IκB kinase (IKK) inhibitor (IC50 = 100 nM). Has no effect on PKA, PKC and CKII activity. Inhibits IκB-α phosphorylation and NFκB activation in HeLa cells. Inhibits NFκB-mediated proinflammatory gene expression in human airway epithelial cells. Enhances TNF-α-induced apoptosis in a multiple myeloma cell line. Attenuates LPS-induced TNF-α production in vivo. Orally active.
Technical Data
| M. Wt | 395.67 |
| Formula | C17H11ClN4O.2HCl |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1049743-58-9 |
| PubChem ID | 16219884 |
| InChI Key | QTDCBADLGJZBHP-UHFFFAOYSA-N |
| Smiles | ClC1=CC(NC(C4=CC=CN=C4)=O)=C(NC3=C2C=CN=C3)C2=C1.Cl.Cl |
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 | 1.98 | 5mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 395.67. 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 | 2.53 mL | 12.64 mL | 25.27 mL |
| 5 mM | 0.51 mL | 2.53 mL | 5.05 mL |
| 10 mM | 0.25 mL | 1.26 mL | 2.53 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.51 mL |
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References
References are publications that support the products' biological activity.
Castro et al (2003) Novel IKK inhibitors: beta-carbolines. Bioorg.Med.Chem.Lett. 13 2419 PMID: 12824047
Newton et al (2007) Repression of inflammatory gene expression in human pulmonary epithelial cells by small-molecule IkappaB kinase inhibitors. J.Pharmacol.Exp.Ther. 321 734 PMID: 17322026
Hideshima et al (2002) NF-kappa B as a therapeutic target in multiple myeloma. J.Biol.Chem. 277 16639 PMID: 11872748
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