RGNCY-0098 (VERU-111 βIII/βIV-tubulin inhibitor)

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VERU-111 is a novel small molecule inhibitor of βIII/βIV-tubulin in pancreatic cancer.  βIII/βIV-tubulin isoforms have been mostly implicated in PanCa progression, metastases and chemo-resistance.  VERU-111 preferentially represses clinically important βIII and βIV tubulin isoforms by restoring miR-200c expression.  Consequently, VERU-111 significantly inhibited tumorigenic and metastatic characteristics of PanCa cells.  VERU-11 also arrested the cell cycle in the G2/M phase and induced apoptosis in the PanCa cells by modulating cell cycle regulatory (Cdc2, Cdc25c, and Cyclin B1) and apoptosis associated (Bax, Bad, Bcl-2 and Bcl-xl) proteins.  In addition, treatment with VERU-111 inhibited tumor growth (P<0.01) in a PanCa xenograft mouse model (AsPC-1).  VERU-11 has significant therapeutic potential in PanCa treatment.

Systematic Name: (2-(1H-indol-3-yl)-1H-imidazol-4-yl)(3,4,5-trimethoxyphenyl)methanone

SMILES:  O=C(C1=CC(OC)=C(OC)C(OC)=C1)C2=CNC(C3=CNC4=CC=CC=C43)=N2

Formula:  C21H19N3O4

Mol Wt:  377.40

PMID:  30674344