同义名 :	-
	CAS号 :	916232-21-8
	货号 :	A1061932
	分子式 :	C28H19FN2O4
	纯度 :	99%+
	分子量 :	466.46
	MDL号 :	MFCD30182334
	存储条件：	Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性

描述

Nuclear factor-kappa B (NF-κB) is known to regulate the expression of divergent genes involved not only in immune and inflammatory responses but also in cell death and survival. IκBα is the protein inhibitor of NF-κB whose phosphorylation is catalyzed by an IκB kinase (abbreviated IKK). GS143 is a selec¬tive IκBα ubiquitination inhibitor with an IC50 of 5.2 μM for SCFβTrCP1-mediated IκBα ubiquitylation. GS143 suppressed the transcription of TNFα-induced NF-κB with a mean IC50 value of 10.5 μM. GS143 also inhibited TNFα-induced expression of ICAM-1 in HT-29 colon cancer cells with an IC50 value of 6.1 μM. The production levels of TNFα and IL-1β in LPS-activated THP-1 cells were inhibited by GS143 with IC50 values of 5.3 μM and 2.1 μM, respectively[2]. In BALB/c mice, intranasal administration of GS143 (16-32 μg/kg) treatment suppressed antigen-induced NF-κB activation in the lung of sensitized mice. GS143 treatment also inhibited antigen-induced eosinophil and lymphocyte recruitment into the airways and the expression of Th2 cytokines and eotaxin in the airways[1].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	2.14mL 0.43mL 0.21mL	10.72mL 2.14mL 1.07mL	21.44mL 4.29mL 2.14mL

参考文献
[1]Hirose K, et al. GS143, an IkappaB ubiquitination inhibitor, inhibits allergic airway inflammation in mice. Biochem Biophys Res Commun. 2008 Sep 26;374(3):507-11 [2]Nakajima H, et al. A novel small-molecule inhibitor of NF-kappaB signaling. Biochem Biophys Res Commun. 2008 Apr 18;368(4):1007-13