Biochem/physiol Actions
Cell penetrant, potent and selective inhibitor of endonuclease activity of CPSF3 in vitro that limits transcriptional termination in cells.
CPSF3-IN-1 (3-(1,3-dihydro-1-hydroxy-2,1-benzoxaborol-7-yl)-N-(40- acetyl-1,10-biphenyl-3-yl) propenamide) is a cell penetrant, potent and selective inhibitor of endonuclease activity of CPSF3 (cleavage and polyadenylation specific factor 3) in vitro that limits transcriptional termination in cells. CPSF3-IN-1 binds to CPSF3 active site and causes transcription readthrough. It potently inhibits growth of numerous cancer cell lines (IC50 = 0.28 µM HCT116 cells).