Biological Activity
Inhibitor of NF-κB activation, possibly via selective inhibition of LPS- and TNF-α-induced IκBα ubiquitination (IC50 = 3 μM). Blocks subsequent production of TNF-α, IL-1β and IL-6. Inhibits mucin production in an in vitro model of COPD, and is anti-inflammatory following oral administration in vivo. Also weakly inhibits EGFR, 5-lipoxygenase and iNOS.
Compound Libraries
Ro 106-9920 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 245.26 |
| Formula | C10H7N5OS |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 62645-28-7 |
| PubChem ID | 3906779 |
| InChI Key | JFSXSNSCPNFCDM-UHFFFAOYSA-N |
| Smiles | O=S(C1=CC=CC=C1)C1=NN2N=NN=C2C=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 | 24.53 | 100 | |
| ethanol | 1.23 | 5 |
Preparing Stock Solutions
The following data is based on the product molecular weight 245.26. 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 | 4.08 mL | 20.39 mL | 40.77 mL |
| 5 mM | 0.82 mL | 4.08 mL | 8.15 mL |
| 10 mM | 0.41 mL | 2.04 mL | 4.08 mL |
| 50 mM | 0.08 mL | 0.41 mL | 0.82 mL |
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References
References are publications that support the products' biological activity.
Conalty et al (1976) Anticancer agents. XII. Pyridazine and benzodiazine derivatives. Proc.R.Ir.Acad.B. 76 151 PMID: 967871
Swinney et al (2002) A small molecule ubiquitination inhibitor blocks NF-κB-dependent cytokine expression in cells and rats. J.Biol.Chem. 277 23573 PMID: 11950839
Baginski et al (2002) Glucocorticoid modulation of MUC5AC secretion in H292 cells. Am.Soc.Cell Biol.Abstr. 765 PMID:
Keywords: Ro 106-9920, supplier, inhibitors, inhibits, NF-κB, NF-kappaB, NF-kB, activation, Transcription, Factors, Nuclear, Factor, Kappa, B, Ro106-9920, NF-kB/IkB, NF-kB/IkB, Tocris Bioscience
