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GS143

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Chemical Structure| 916232-21-8 同义名 : -
CAS号 : 916232-21-8
货号 : A1061932
分子式 : C28H19FN2O4
纯度 : 99%+
分子量 : 466.46
MDL号 : MFCD30182334
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(75.03 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Nuclear factor-kappa B (NF-κB) is known to regulate the expression of divergent genes involved not only in immune and inflammatory responses but also in cell death and survival. IκBα is the protein inhibitor of NF-κB whose phosphorylation is catalyzed by an IκB kinase (abbreviated IKK). GS143 is a selec¬tive IκBα ubiquitination inhibitor with an IC50 of 5.2 μM for SCFβTrCP1-mediated IκBα ubiquitylation. GS143 suppressed the transcription of TNFα-induced NF-κB with a mean IC50 value of 10.5 μM. GS143 also inhibited 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 were inhibited by GS143 with IC50 values of 5.3 μM and 2.1 μM, respectively[2]. In BALB/c mice, intranasal administration of GS143 (16-32 μg/kg) treatment suppressed antigen-induced NF-κB activation in the lung of sensitized mice. GS143 treatment also inhibited antigen-induced eosinophil and lymphocyte recruitment into the airways and the expression of Th2 cytokines and eotaxin in the airways[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.14mL

0.43mL

0.21mL

10.72mL

2.14mL

1.07mL

21.44mL

4.29mL

2.14mL
参考文献

[1]Hirose K, et al. GS143, an IkappaB ubiquitination inhibitor, inhibits allergic airway inflammation in mice. Biochem Biophys Res Commun. 2008 Sep 26;374(3):507-11

[2]Nakajima H, et al. A novel small-molecule inhibitor of NF-kappaB signaling. Biochem Biophys Res Commun. 2008 Apr 18;368(4):1007-13