Orally active, ATP-competitive IKKβ inhibitor (IC50 = 3 - 12 μM) that displays > 10-fold selectivity over 28 other kinases including JNK, p38, MK2 and ERK. Attenuates NF-κB-induced gene expression of IL-6, IL-8 and COX-2 in synovial fibroblasts (IC50 values are 20, 20 and 8 μM respectively). Reduces iNOS induction and exhibits anti-inflammatory activity in vivo.
Sold for research purposes under agreement from AstraZeneca
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 224.3. 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||4.46 mL||22.29 mL||44.58 mL|
|5 mM||0.89 mL||4.46 mL||8.92 mL|
|10 mM||0.45 mL||2.23 mL||4.46 mL|
|50 mM||0.09 mL||0.45 mL||0.89 mL|
The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.
References are publications that support the products' biological activity.
Kishore et al (2003) A selective IKK-2 inhibitor blocks NF-κB-dependent gene expression in interleukin-1β-stimulated synovial fibroblasts. J.Biol.Chem. 278 32861 PMID: 12813046
Gomez et al (2005) Selective inhibition of kappa B kinase-β aborgates induction of nitric oxide synthase in lipopolysaccharide-stimulated rat aortic smooth muscle cells. Br.J.Pharmacol. 146 217 PMID: 15997236
If you know of a relevant reference for SC 514, please let us know.
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Keywords: IKK-2 inhibitors inhibits attenuates NF-κB NF-kappaB-induced gene expression NF-kB IKK IκB IkappaB Kinases Nuclear Factor Kappa B NF-kappaB Cytokine Signaling Signalling Transcription Factors SC514 AstraZeneca IkB Kinase
1 Citation for SC 514
Citations are publications that use Tocris products. Selected citations for SC 514 include:
Akhtar et al (2015) MicroRNA-602 and microRNA-608 regulate sonic hedgehog expression via target sites in the coding region in human chondrocytes. Nature 67 423 PMID: 25385442
Do you know of a great paper that uses SC 514 from Tocris? If so please let us know.