Description: Selective IKK inhibitor; orally active
Chemical Name:N-(6-Chloro-9H-pyrido[3,4-b]indol-8-yl)-3-pyridinecarboxamide dihydrochloride
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
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.
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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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Newtonet 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
Hideshimaet al (2002) NF-kappa B as a therapeutic target in multiple myeloma. J.Biol.Chem. 277 16639 PMID: 11872748