Home / Ubiquitin Ligase (E3) Inhibitors / GS 143

GS 143

Catalog #: 5636
2 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
5636/50
5636/10
GS 143 | CAS No. 916232-21-8 | Ubiquitin Ligase (E3) Inhibitors
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Description: β-TrCP1 ligase inhibitor

Chemical Name: 4-[4-[[5-(2-Fluorophenyl)-2-furanyl]methylene]-4,5-dihydro-5-oxo-3-(phenylmethyl)-1H-pyrazol-1-yl]benzoic acid

Purity: ≥98%

Product Details
Citations (2)
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

GS 143 is a β-TrCP1 ligase inhibitor. Inhibits IκBα ubiquitination (IC50 = 5.2 μM) without affecting proteasome activity. Blocks LPS-induced expression of inflammatory cytokines in human myelomonocytic cells. Suppresses antigen-induced NFκB expression, inflammation and mucus production in airways of OVA-sensitized mice.

Technical Data

M.Wt:
466.46
Formula:
C28H19FN2O4
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at +4°C
CAS No:
916232-21-8

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. GS143, an IκB ubiquitination inhibitor, inhibits allergic airway inflammation in mice.
    Hirose et al.
    Biochem.Biophys.Res.Comm., 2008;374:507
  2. A novel small-molecule inhibitor of NF-κB signaling.
    Nakajima et al.
    Biochem.Biophys.Res.Comm., 2008;368:1007
  3. Progesterone receptor membrane component 1 leads to erlotinib resistance, initiating crosstalk of Wnt/&beta-catenin and NF-&kappaB pathways, in lung adenocarcinoma cells
    Y Lin, K Higashisak, T Shintani, A Maki, S Hanamuro, Y Haga, S Maeda, H Tsujino, K Nagano, Y Fujio, Y Tsutsumi
    Sci Rep, 2020;10(1):4748.

Product Datasheets

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Citations for GS 143

The citations listed below are publications that use Tocris products. Selected citations for GS 143 include:

2 Citations: Showing 1 - 2

  1. SKI activates the Hippo pathway via LIMD1 to inhibit cardiac fibroblast activation.
    Authors: Robert R Et al.
    Basic Res Cardiol  2021;116:25
  2. Periostin in cardiovascular disease and development: a tale of two distinct roles.
    Authors: Smadar Et al.
    Basic Res Cardiol  2018;113:1

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