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. 2018 Nov 8;9(12):1181–1185. doi: 10.1021/acsmedchemlett.8b00323

Figure 2.

Figure 2

In vitro hit validation. (a) Structures and inhibitory activities of the hit analogues. EMSA was performed by using Lin28a–preE-let-7g pair. (b) KCB3602 promoted let-7 maturation at the Dicer assay. (c) SPR analysis to detect direct binding event between Lin28a and KCB3602 at various concentrations ranging from 0.31 to 10 μM. Inset shows the dose–response curve. Calculated Rmax is 43. (d) RNA pull-down assay using 5′-biotinylated preE-let-7g and proteome from JAR human choriocarcinoma cells to check the target engagement at the cellular context.