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.

Product information

CAS Number: 2024548-03-4

Molecular Weight: 583.59

Formula: C31H29N5O7

Chemical Name: 4-(7-{4-[(benzyloxy)carbonyl]piperazin-1-yl}-4,4-dimethyl-8-nitro-1H,4H-chromeno[4,3-c]pyrazol-1-yl)benzoic acid

Smiles: CC1(C)OC2=CC(=C(C=C2C2=C1C=NN2C1C=CC(=CC=1)C(O)=O)[N+]([O-])=O)N1CCN(CC1)C(=O)OCC1C=CC=CC=1

InChiKey: GBHKWXUSQTVIBN-UHFFFAOYSA-N

InChi: InChI=1S/C31H29N5O7/c1-31(2)24-18-32-35(22-10-8-21(9-11-22)29(37)38)28(24)23-16-26(36(40)41)25(17-27(23)43-31)33-12-14-34(15-13-33)30(39)42-19-20-6-4-3-5-7-20/h3-11,16-18H,12-15,19H2,1-2H3,(H,37,38)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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.

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