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GS143

CAS No. : 916232-21-8

MCE 站：GS143

产品活性：GS143 是一种选择性的 IκBα 泛素化抑制剂，对于 SCF^βTrCP1 介导的 IκBα 泛素化作用的 IC₅₀ 为 5.2 μM。GS143 抑制靶基因的 NF-κB 活化和转录，并且不抑制蛋白酶体的活性，并具有抗哮喘作用。

研究领域：NF-κB  |  Metabolic Enzyme/Protease

作用靶点：IKK  |  E1/E2/E3 Enzyme  |  NF-κB

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 pro?duc?tion in Th2-polar?iz?ing con?di?tion is mark?edly sup?pressed by GS143 in a dose-depen?dent man?ner.
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.

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.

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