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。
| 生物活性 | GS143 is a selec-tiveIκBα ubiquitinationinhibitor with anIC50of 5.2 μM for SCFβTrCP1-mediatedIκBα ubiquitylation. GS143 sup-pressesNF-κBacti-va-tion and tran-scrip-tion of tar-get genes and does not inhibitproteasomeactivity. GS143 has anti-asthma effect[1][2]. |
| IC50& Target | IC50: 5.2 μM (SCFβTrCP1-mediated IκBα ubiquitylation)[2] |
体外研究
(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[1].
GS143 suppresses the transcription of TNFα-induced NF-κB with a mean IC50value of 10.5 μM. GS143 also inhibits TNFα-induced expression of ICAM-1 in HT-29 colon cancer cells with an IC50value of 6.1 μM. The production levels of TNFα and IL-1β in LPS-activated THP-1 cells are inhibited with IC50values of 5.3 μM and 2.1 μM, respectively. GS143 does not inhibit p53 and β-catenin[2].
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体内研究
(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[1].
| Animal Model: | BALB/c mice (age 7-8weeks) injected with oval-bu-min[1] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 37.5 mg/mL(80.39 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 2.1438 mL | 10.7190 mL | 21.4381 mL | | 5 mM | 0.4288 mL | 2.1438 mL | 4.2876 mL | | 10 mM | 0.2144 mL | 1.0719 mL | 2.1438 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: 2.08 mg/mL (4.46 mM); Clear solution; Need ultrasonic
此方案可获得 2.08 mg/mL (4.46 mM) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: 1.88 mg/mL (4.03 mM); Suspended solution; Need ultrasonic
此方案可获得 1.88 mg/mL (4.03 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 18.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 *以上所有助溶剂都可在本网站选购。
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