Custom Premix Selecting "Custom Premix" option means that all of the beads you have chosen will be premixed in manufacturing before the kit is sent to you.
A cell-permeable tetrazolopyridazine-phenylsulfoxide compound that displays anti-inflammatory properties. Acts as a highly selective, irreversible inhibitor of IκBαee ubiquitination (IC50 = 2.3 µM). Blocks NF-κB-dependent cytokine expression in human PBMNs (IC50’s = ~ 700 nM for TNF-α, IL-1β, and IL-6 inhibition) and rats. Does not inhibit SCFβTRCP(IκBα ubiquitin ligase)-mediated β-catenin ubiquitination in Jurkat cells. At 10 µM concentrations, also inhibits the activities of 5-lipoxygenase (by 89%) and EGFR kinase (by 63%).
Catalogue Number
557550
Brand Family
Calbiochem®
References
References
Swinney, D.C., et al. 2002. J. Biol. Chem.277, 23573.
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
Revision
30-April-2009 JSW
Description
A cell-permeable tetrazolopyridazine-phenylsulfoxide compound that displays anti-inflammatory properties. Acts as a highly selective, irreversible inhibitor of IκBαee ubiquitination (IC50 = 2.3 µM). Also reported to prevent degradation of IκBαee in MM6 cells (complete inhibition at ~3-5 µM). Shown to block NF-κB-dependent cytokine expression in human peripheral blood mononuclear cells (PBMN) (IC50 = 600-700 nM for TNF-α, IL-1β, and IL-6 inhibition). Also shown to lower circulating levels of TNFα in LPS-treated rats. Also shown to inhibit 5-lipoxygenase (89% inhibition) and EGFR kinase (63% inhibition) at higher concentrations (10 µM).
Form
White solid
Intert gas (Yes/No)
Packaged under inert gas
CAS number
62645-28-7
Chemical formula
C₁₀H₇N₅OS
Structure formula
Purity
≥95% by HPLC
Solubility
DMSO (25 mg/ml) or Ethanol (1 mg/ml)
Storage
Protect from moisture
Protect from light
≤ -70°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 3 months at -70°C.
Toxicity
Standard Handling
References
Swinney, D.C., et al. 2002. J. Biol. Chem.277, 23573.
