1. NF-κB
    Metabolic Enzyme/Protease
  2. IKK
    E1/E2/E3 Enzyme
    NF-κB
  3. GS143

GS143 

Cat. No.: HY-110261
Handling Instructions

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.

For research use only. We do not sell to patients.

GS143 Chemical Structure

GS143 Chemical Structure

CAS No. : 916232-21-8

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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].

IC50 & 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.
Molecular Weight

466.46

Formula

C₂₈H₁₉FN₂O₄

CAS No.

916232-21-8

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

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

GS143GS 143GS-143IKKE1/E2/E3 EnzymeNF-κBIκB kinaseI kappa B kinase E1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseNuclear factor-κBNuclear factor-kappaBIκBαubiquitinationanti-asthmaeosinophilTh2airwayinflammationIL-4βTrCP1Inhibitorinhibitorinhibit

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