Lin28-let-7a antagonist 1 shows a clear antagonistic effect against the Lin28-let-7a interaction with an IC₅₀ of 4.03 μM for Lin28A-let-7a-1 interaction.

IC50：4.03 μM (Lin28A-let-7a-1)^[1].

Lin28-let-7a antagonist 1 (compound 1) shows a clear antagonistic effect against the Lin28A-let-7a-1 interaction with an IC₅₀ of 4.03 μM. Interestingly, Lin28-let-7a antagonist 1 also inhibits the Lin28B-let-7 interaction, with slightly reduced potency. Dicer processing assay reveals that Lin28-let-7a antagonist 1 clearly blocks the formation of the Lin28A-pre-let-7g complex and induces miRNA processing, resulting in the generation of mature let-7g miRNA. When the expression of both Lin28A and Lin28B are knocked-down using siRNA in JAR cells, the Lin28-let-7a antagonist 1-induced increase in cellular let-7 levels is clearly attenuated. Lin28A-let-7a-IN-1 increases mature let-7 levels in PA-1 cells that express high level of Lin28A. On the other hand, let-7 levels are not affected by 1 in MCF7 cells that rarely express Lin28 proteins. Taken together, Lin28-let-7a antagonist 1 specifically induces the increase in the cellular let-7 levels by targeting Lin28^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

583.59

C₃₁H₂₉N₅O₇

2024548-03-4

Room temperature in continental US; may vary elsewhere.

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

In Vitro: 

DMSO : 100 mg/mL (171.35 mM; Need ultrasonic)

*

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

• [1]. Lim D, et al. Discovery of a Small-Molecule Inhibitor of Protein-MicroRNA Interaction Using Binding Assay with a Site-Specifically Labeled Lin28. J Am Chem Soc. 2016 Oct 7.