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Lin28-let-7a antagonist 1

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Chemical Structure| 2024548-03-4 同义名 : -
CAS号 : 2024548-03-4
货号 : A462770
分子式 : C31H29N5O7
纯度 : 99%+
分子量 : 583.591
MDL号 : MFCD30741839
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: 105 mg/mL(179.92 mM)，配合低频超声助溶，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 MicroRNAs (miRNAs) are small noncoding RNAs that play important roles in posttranscriptional gene regulation. In animal cells, miRNAs regulate their targets by translational inhibition and mRNA destabilization[1]. Currently, there are over 1000 known human microRNAs, and microRNAs control over 50% of mammalian protein coding genes[2]. MicroRNAs act to decrease the expression of messenger RNAs that contain stretches of sequence complementary to the microRNA[3].MiRNA targeting is defined by the complementarities between positions 2-8 of miRNA 5'-end with generally the 3'-untranslated region of target mRNAs (messenger RNAs). The capacity of miRNAs to simultaneously inhibit many different mRNAs allows for an amplification of biological responses[4].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. 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[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.71mL

0.34mL

0.17mL

8.57mL

1.71mL

0.86mL

17.14mL

3.43mL

1.71mL
参考文献

[1]Natascha Bushati,et al. microRNA functions. Annu Rev Cell Dev Biol. 2007;23:175-205.

[2]Bridget Simonson, Saumya Das . MicroRNA Therapeutics: the Next Magic Bullet? Mini Rev Med Chem. 2015;15(6):467-74.

[3]Ashley M Mohr,et al. Overview of microRNA biology. Semin Liver Dis. 2015 Feb;35(1):3-11.

[4]David Mellis,et al. MicroRNA-based therapeutics in cardiovascular disease: screening and delivery to the target. Biochem Soc Trans. 2018 Feb 19;46(1):11-21.

[5] 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.