916232-21-8
916232-21-8 結(jié)構(gòu)式
基本信息
4-(3-芐基-4-((5-(2-氟苯基)呋喃-2-基)亞甲基)-5-氧代-4,5-二氫-1H-吡唑-1-基)苯甲酸
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
物理化學(xué)性質(zhì)
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)
常見問題列表
IC50: 5.2 μM (SCF βTrCP1 -mediated IκBα ubiquitylation)
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 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.
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 oval-bu-min |
| 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. |