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.
CAS Number: 916232-21-8
Molecular Weight: 466.46
Chemical Name: 4-(3-benzyl-4-((5-(2-fluorophenyl)furan-2-yl)methylene)-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
GS143 was used at 10-20 µM final concentration in various assays.
OVA-sensitized mice were given intranasally with GS143 (16 or 32 µg) and 2 h later, these mice were challenged with inhaled OVA.
- Hirose K, et al. GS143, an IkappaB ubiquitination inhibitor, inhibits allergic airway inflammation in mice. Biochem Biophys Res Commun. (2008) 374(3):507-11.
- 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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