GS143, IkappaB Ubiquitination Inhibitor


Catalog No. size PriceQuantity
M60308-2S 2 mg solid $129
M60308-10S 10mg solid $529

Description

Product Information
Molecular Weight: 466.46
Formula: C28H19FN2O4
Purity: ≥98%
CAS#: 916232-21-8
Solubility: DMSO up to 100 mM
Chemical Name: 4-(3-benzyl-4-((5-(2-fluorophenyl)furan-2-yl)methylene)-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

 

Biological Activity:

GS143 is selective β-TrCP1 ligase inhibitor, inhibits IκBα ubiquitination with IC50 ~5.2 μM without affecting proteasome activity. It blocks LPS-induced expression of inflammatory cytokines in human myelomonocytic cells. It suppresses antigen-induced NFκB expression, inflammation and mucus production in airways of OVA-sensitized mice.

How to Use:

In vitro: GS143 was used at 10-20 µM final concentration in various assays.
In vivo: OVA-sensitized mice were given intranasally with GS143 (16 or 32 µg) and 2 h later, these mice were challenged with inhaled OVA.

Reference:

  • 1. Hirose K, et al. GS143, an IkappaB ubiquitination inhibitor, inhibits allergic airway inflammation in mice. Biochem Biophys Res Commun. (2008) 374(3):507-11.
  • 2. Nakajima H, et al. A novel small-molecule inhibitor of NF-kappaB signaling. (2008) Biochem Biophys Res Commun. 368(4):1007-13.


Products are for research use only. Not for human use.

 

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