916232-21-8

中文名称 4-(3-苄基-4-((5-(2-氟苯基)呋喃-2-基)亚甲基)-5-氧代-4,5-二氢-1H-吡唑-1-基)苯甲酸

英文名称 GS 143

CAS 916232-21-8

分子式 C28H19FN2O4

分子量 466.46

MOL 文件 916232-21-8.mol

更新日期 2024/03/06 11:25:46

916232-21-8 结构式

基本信息物理化学性质安全数据图谱信息常见问题列表

基本信息

中文别名

化合物GS-143
4-(3-苄基-4-((5-(2-氟苯基)呋喃-2-基)亚甲基)-5-氧代-4,5-二氢-1H-吡唑-1-基)苯甲酸

英文别名

GS 143
4-(3-Benzyl-4-{[5-(2-fluorophenyl)furan-2-yl]methylidene}-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
4-[4-[[5-(2-Fluorophenyl)-2-furanyl]methylene]-4,5-dihydro-5-oxo-3-(phenylmethyl)-1H-pyrazol-1-yl]benzoic acid
E2 conjugating enzyme,inhibit,IκBα,Th2,Ubiquitin conjugating enzyme,GS143,Ubiquitin ligase,IL-4,IκB kinase,βTrCP1,Nuclear factor-kappaB,eosinophil,Ubiquitin activating enzyme,Nuclear factor-κB,I kappa B kinase,NF-κB,E3 ligating enzyme,IKK,E1 activating enzyme,anti-asthma,E1/E2/E3 Enzyme,ubiquitination,Inhibitor,airway,inflammation

物理化学性质

储存条件2-8°C

储存条件Sealed in dry,2-8°C

溶解度DMF:25.0(Max Conc. mg/mL);53.59(Max Conc. mM)
DMF:PBS (pH 7.2) (1:4):0.2(Max Conc. mg/mL);0.43(Max Conc. mM)
DMSO:31.38(Max Conc. mg/mL);67.28(Max Conc. mM)

形态结晶固体

安全数据

危险性符号(GHS)

GHS07

警示词警告

危险性描述H302-H315-H319-H335

防范说明P261-P305+P351+P338

图谱信息

4-(3-苄基-4-((5-(2-氟苯基)呋喃-2-基)亚甲基)-5-氧代-4,5-二氢-1H-吡唑-1-基)苯甲酸(916232-21-8)核磁图(¹HNMR)

常见问题列表

生物活性

GS143 是一种选择性的 IκBα 泛素化抑制剂，对于 SCFβTrCP1 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。

靶点

IC50: 5.2 μM (SCF ^βTrCP1 -mediated IκBα ubiquitylation)

体外研究

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.
GS143 suppresses the transcription of TNFα-induced NF-κB with a mean IC ₅₀ value of 10.5 μM. GS143 also inhibits TNFα-induced expression of ICAM-1 in HT-29 colon cancer cells with an IC ₅₀ value of 6.1 μM. The production levels of TNFα and IL-1β in LPS-activated THP-1 cells are inhibited with IC ₅₀ values of 5.3 μM and 2.1 μM, respectively. GS143 does not inhibit p53 and β-catenin.

体内研究

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.

Animal Model:	BALB/c mice (age 7-8weeks) injected with ovalbumin
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.