产品详情
简单介绍：
GS143,IkappaBUbiquitinationInhibitor
详情介绍：
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:
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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