CBA-1 is a small molecule inhibitor of Wnt signaling, specifically targets Jumonji (JmjC) domain-containing demethylase KDM3A with IC50 of 3.9 uM.
CBA-1 also poorly inhibited KDM3B.
CBA-1 (3 μM) inhibited Wnt signaling induced by either LiCl or Wnt proteinin TOPFlash reporter assays, repressed the expression of Wnt target genes and inhibited cell proliferation in CRC cells, inhibited colon cancer organoids formation.
The binding affinity of CBA-1 to KDM3A is greater than that of GSK-J1, CBA-1 was a better Wnt inhibitor than either GSK-J1 or GSK-J4.
CBA-1 showed no clear effects on the assembly of β-catenin/TCF.
CBA-1 inhibited Wnt signaling in the tail of Wnt/β-catenin zebrafish reporter line.
CBA-1 (5 and 10 μM) was able to rescue completely the loss-of-eye phenotype in zebrafish.
