RGNCY-0070 (BTYNB IMP1 inhibitor)

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BTYNB is a potent and selective inhibitor of IMP1 binding to c-Myc mRNA.  BTYNB down regulates several mRNA transcripts regulated by IMP1 in cells.  BTYNB detabilises c-Myc mRNA resulting in the down regulation of c-Myc mRNA and protein.  It also down regulates β-TrCP1 mRNA and reduces activation of nuclear transcriptional factors-Kappa B (NF-kB).  BTYNB potently inhibited proliferation of IMP1 containing ovarian cancer and melanoma cells with no effect in IMP1 negative cells.  The overexpression of IMP1 reverses BTYNB inhibition of cell proliferation.  In addition, BTYNB completely blocked anchorage independent growth of melanoma and ovarian cancer cells in colony formation assays.  BTYNB has a unique mode of action and its ability to inhibit cancer cell proliferation makes it a candidate for further therapeutic evaluation.  IMP1 binding to c-Myc mRNA (IC50=5μM).

SMILE:  BrC1=CC=C(/C=N/C2=CC=CC=C2C(N)=O)S1

Systematic Name:  (E)-2-(((5-bromothiophen-2-yl)methylene)amino)benzamide

Molecular Weight: 309.18

Formula:  C12H9BrN2OS

PMID:  28846937