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CBA-1

Chemical Structure : CBA-1

CAS No.: 333318-69-7

CBA-1 (KDM3A inhibitor CBA-1)

Catalog No.: PC-20353Not For Human Use, Lab Use Only.

CBA-1 is a small molecule inhibitor of Wnt signaling, specifically targets Jumonji (JmjC) domain-containing demethylase KDM3A with IC50 of 3.9 uM.

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    Biological Activity

    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.

    Physicochemical Properties

    M.Wt 425.96
    Formula C24H28ClN3O2
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    N-((5-chloro-8-hydroxyquinolin-7-yl) (4-(diethylamino)phenyl)-methyl)butyramide

    References

    1. Wen Zhang, et al. iScience. 2020 Nov 13;23(12):101795.

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