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Lin28-let-7a antagonist 1

Catalog No.GC30501

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.

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Lin28-let-7a antagonist 1 Chemical Structure

Cas No.: 2024548-03-4

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Sample solution is provided at 25 µL, 10mM.

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Background

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.

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].

[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.

Chemical Properties

Cas No. 2024548-03-4 SDF
Canonical SMILES O=C(O)C(C=C1)=CC=C1N2N=CC3=C2C4=CC([N+]([O-])=O)=C(N5CCN(C(OCC6=CC=CC=C6)=O)CC5)C=C4OC3(C)C
Formula C31H29N5O7 M.Wt 583.59
Solubility Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

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1 mg 5 mg 10 mg
1 mM 1.7135 mL 8.5677 mL 17.1353 mL
5 mM 0.3427 mL 1.7135 mL 3.4271 mL
10 mM 0.1714 mL 0.8568 mL 1.7135 mL
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