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GS-143
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
GS-143图片
CAS NO:916232-21-8
包装与价格：
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
GS-143 是一种选择性 IκBα 泛素化抑制剂，对 SCFβTrCP1 介导的 IκBα 泛素化的 IC50 为 5.2 μM。
Cas No.916232-21-8
别名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
化学名4-[4-[[5-(2-fluorophenyl)-2-furanyl]methylene]-4,5-dihydro-5-oxo-3-(phenylmethyl)-1H-pyrazol-1-yl]-benzoic acid
Canonical SMILESO=C1N(C2=CC=C(C(O)=O)C=C2)N=C(CC3=CC=CC=C3)/C1=C\C4=CC=C(C5=CC=CC=C5F)O4
分子式C28H19FN2O4
分子量466.5
溶解度10mg/mL in DMSO, 25mg/mL in DMF
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

GS-143 is an inhibitor of IκBα ubiquitylation.[1] It inhibits ubiquitylation of phosphorylated IκBα mediated by the SCFβTrCP1 E3 ubiquitin ligase complex in vitro (IC50 = 5.2 μM) and reduces TNF-α-induced degradation of phosphorylated IκBα, but not β-catenin, another SCFβTrCP1 substrate, in HeLa S3 cells. GS-143 inhibits LPS-induced expression of TNF-α, IL-6, IL-12, ICAM-1, and NF-κB in THP-1 cells in a concentration-dependent manner. Intranasal administration of GS-143 (32 μg/animal) reduces the number of eosinophils, lymphocytes, and total cells in bronchoalveolar lavage fluid (BALF) in an ovalbumin-sensitized mouse model of allergic asthma.[2]

Reference:
[1]. Nakajima, H., Fujiwara, H., Furuichi, Y., et al. A novel small-molecule inhibitor of NF-κB signaling. Biochem. Biophys. Res. Commun. 368(4), 1007-1013 (2008).
[2]. Hirose, K., Wakashin, H., Oki, M., et al. GS143, an IκB ubiquitination inhibitor, inhibits allergic airway inflammation in mice. Biochem. Biophys. Res. Commun. 374(3), 507-511 (2008).