GS143 is a selec-tiveIκBα ubiquitinationinhibitor with anIC₅₀of 5.2 μM for SCF^βTrCP1-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: 5.2 μM (SCF^βTrCP1-mediated IκBα ubiquitylation)^[2]

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].

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].

466.46

Solid

C₂₈H₁₉FN₂O₄

916232-21-8

Room temperature in continental US; may vary elsewhere.

DMSO : 37.5 mg/mL(80.39 mM;ultrasonic and warming and heat to 60℃)

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。

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。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液