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GS-143

  Cat. No.:  DC39001   Featured
Chemical Structure
916232-21-8
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More than 5000 active chemicals with high quality for research!
Field of application
GS-143 is an inhibitor of IκBα ubiquitylation. 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.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 916232-21-8
Chemical Name: 4-[4-[[5-(2-Fluorophenyl)-2-furanyl]methylene]-4,5-dihydro-5-oxo-3-(phenylmethyl)-1H-pyrazol-1-yl]benzoic acid
Synonyms: GS-143; GS 143; GS143;
SMILES: FC(C=CC=C1)=C1C2=CC=C(O2)/C=C3C(CC4=CC=CC=C4)=NN(C5=CC=C(C(O)=O)C=C5)C\3=O
Formula: C28H19FN2O4
M.Wt: 466.46
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: 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).
Description: GS143 is a selec­tive IκBα ubiquitination inhibitor with an IC50 of 5.2 μM for SCFβTrCP1-mediated IκBα ubiquitylation. GS143 sup­presses NF-κB acti­va­tion and tran­scrip­tion of tar­get genes and does not inhibit proteasome activity. GS143 has anti-asthma effect[1][2].
Target: IC50: 5.2 μM (SCFβTrCP1-mediated IκBα ubiquitylation)[2]
In Vivo: GS143 (16-32 μg/body; intranasal administration; once; BALB/c mice) treatment suppresses antigen-induced NF-κB activation in the lung of sensitized mice. GS143 treatment also inhibits antigen-induced eosinophil and lymphocyte recruitment into the airways and the expression of Th2 cytokines and eotaxin in the airways[1]. Animal Model: BALB/c mice (age 7-8weeks) injected with oval­bu­min[1] Dosage: 16 μg/body or 32 μg/body Administration: Intranasal administration; once Result: Suppressed antigen-induced NF-κB activation in the lung of sensitized mice.
In Vitro: GS143 (10 μM or 20 μM) inhibits antigen-induced differentiation of Th2 cells but not of Th1 cells in vitro. The IL-4 pro­duc­tion in Th2-polar­iz­ing con­di­tion is mark­edly sup­pressed by GS143 in a dose-depen­dent man­ner[1]. GS143 suppresses the transcription of TNFα-induced NF-κB with a mean IC50 value of 10.5 μM. GS143 also inhibits 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 are inhibited with IC50 values of 5.3 μM and 2.1 μM, respectively. GS143 does not inhibit p53 and β-catenin[2].
References: [1]. Koichi Hirose, 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]. Hiroto Nakajima, et al. A novel small-molecule inhibitor of NF-kappaB signaling. Biochem Biophys Res Commun. 2008 Apr 18;368(4):1007-13.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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