Biological Activity
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.
Licensing Information
Sold for research purposes under agreement from AstraZeneca
Technical Data
| M. Wt | 224.3 |
| Formula | C9H8N2OS2 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 354812-17-2 |
| PubChem ID | 2807869 |
| InChI Key | BMUACLADCKCNKZ-UHFFFAOYSA-N |
| Smiles | NC1=C(C(N)=O)SC(C2=CSC=C2)=C1 |
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 | 22.43 | 100 | |
| ethanol | 2.24 | 10 |
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 |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
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
Baxter et al (2004) Hit-to-lead studies: the discovery of potent, orally active thiophenecarboxamide IKK-2 inhibitors. Bioorg.Med.Chem.Letts. 14 2817 PMID:
Keywords: SC 514, supplier, 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, NF-kB/IkB, IkB, Kinase, IkB, Kinase, Tocris Bioscience
