GS-143 |
Catalog No.GC43786 |
GS-143 est un inhibiteur sélectif de l'ubiquitination IκBα avec une IC50 de 5,2 μM pour l'ubiquitylation IκBα médiée par SCFβTrCP1.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 916232-21-8
Sample solution is provided at 25 µL, 10mM.
GS-143 is an inhibitor of IκBα ubiquitylation.[1] It inhibits ubiquitylation of phosphorylated IκBα mediated by the SCFβTrCP1 E3 ubiquitin ligase complex in vitro (IC50 = 5.2 μM) and reduces TNF-α-induced degradation of phosphorylated IκBα, but not β-catenin, another SCFβTrCP1 substrate, in HeLa S3 cells. GS-143 inhibits LPS-induced expression of TNF-α, IL-6, IL-12, ICAM-1, and NF-κB in THP-1 cells in a concentration-dependent manner. Intranasal administration of GS-143 (32 μg/animal) reduces the number of eosinophils, lymphocytes, and total cells in bronchoalveolar lavage fluid (BALF) in an ovalbumin-sensitized mouse model of allergic asthma.[2]
Reference:
[1]. Nakajima, H., Fujiwara, H., Furuichi, Y., et al. A novel small-molecule inhibitor of NF-κB signaling. Biochem. Biophys. Res. Commun. 368(4), 1007-1013 (2008).
[2]. Hirose, K., Wakashin, H., Oki, M., et al. GS143, an IκB ubiquitination inhibitor, inhibits allergic airway inflammation in mice. Biochem. Biophys. Res. Commun. 374(3), 507-511 (2008).
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