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GS143,IkappaBUbiquitinationInhibitor

品牌：Xcessbio

貨號：M60308-2s

規(guī)格：2 mg solid

貨期：

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GS143,IkappaBUbiquitinationInhibitor

商品詳情參考文獻相關資料

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: 4^oC 1 year. DMSO: 4^oC 3 month; -20^oC 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.

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