MDK6620 is a potent and selective IMP1 inhibitor by inhibiting IMP1 binding to c-Myc mRNA with IC50 value of 5μM. It downregulates several mRNA transcripts regulated by IMP1, resulting in downregulation of c-Myc mRNA and protein, including c-Myc mRNA, β-TrCP1 mRNA, eEF2 mRNA, as well as reducing activation of NF-κB.
BTYNB is a potent and selective inhibitor of IMP1 binding to c-Myc mRNA (IC50=5 μM). BTYNB exhibits selectivity and effectiveness against IMP1-postive cancer cell lines. BTYNB elicits a robust dose-dependent inhibition of cell proliferation in IMP1-positive cells with IC50 values of 2.3 μM, 3.6 μM, and 4.5 μM in ES-2, IGROV-1, and SK-MEL2 cells, respectively. Pretreatment with 10μM BTYNB for 72 hours enhances the degradation rate of c-Myc mRNA in SK-MEL2 cells[2]. Through impairing IGF2BP1-RNA association, BTYNB could disrupt the stabilization of E2F-driven transcripts by IGF2BP1 in cancer[3].
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