916232-21-8

916232-21-8 structure

Name: GS143
Chemical Name: GS-143
CAS Number: 916232-21-8
Molecular Formula: C₂₈H₁₉FN₂O₄
Molecular Weight: 466.5
Catalog: Signaling Pathways Metabolic Enzyme/Protease E1/E2/E3 Enzyme
Create Date: 2020-09-24 18:02:04
Modify Date: 2024-01-31 21:22:49
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].

Name	GS-143
Synonyms	MFCD30182334

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].
Related Catalog	Signaling Pathways >> NF-κB >> IKK Signaling Pathways >> Metabolic Enzyme/Protease >> E1/E2/E3 Enzyme Research Areas >> Inflammation/Immunology
Target	IC50: 5.2 μM (SCFβTrCP1-mediated IκBα ubiquitylation)[2]
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].
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.
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.

Molecular Formula	C₂₈H₁₉FN₂O₄
Molecular Weight	466.5
Appearance	A crystalline solid
Storage condition	Store at +4°C

Hazard Codes	Xi

1158522-08-7	940364-43-2
134104-43-1	131615-57-1
6906-52-1	930439-75-1
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849349-65-1	127437-46-1