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E722-2648

Chemical Structure : E722-2648

CAS No.: 931963-55-2

E722-2648 (β-catenin/BCL9 inhibitor C1)

Catalog No.: PC-38567Not For Human Use, Lab Use Only.

E722-2648 (Compound C-1) is a novel specific and competitive small molecule β-catenin/BCL9 interaction inhibitor with ITC KD of 1.05 uM and IC50 of 9 uM, blocks oncogenic Wnt signaling and disrupts cholesterol homeostasis in colorectal cancer.

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    Biological Activity

    E722-2648 (Compound C-1) is a novel specific and competitive small molecule β-catenin/BCL9 interaction inhibitor with ITC KD of 1.05 uM and IC50 of 9 uM, blocks oncogenic Wnt signaling and disrupts cholesterol homeostasis in colorectal cancer.
    E722-2648 (Compound C-1) inhibited β-catenin/BCL9 complexes at concentrations as low as 1 uM in BCL9-dependent CRC cell lines, Colo320 and HCT116.
    E722-2648 (Compound C-1) inhibited the expression of bona fide downstream Wnt/β-catenin target genes, AXIN2 and CD44, in the β-catenin/BCL9-dependent CRC cell lines.
    E722-2648 (Compound C-1) disrupted cholesterol homeostasis via increased cholesterol esterification and lipid droplet accumulation.
    E722-2648 (Compound C-1) demonstrated antitumorigenic activity in CRC cell lines and xenograft mouse models.

    Physicochemical Properties

    M.Wt 390.604
    Formula C21H30N2OS2
    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-(3-(3-methylpiperidin-1-yl)propyl)-6,7,8,9-tetrahydro-1H-benzo[4,5]thieno[3,2-c]thiopyran-3-carboxamide

    References

    1. Helen Tanton, et al. Sci Adv. 2022 Apr 29;8(17):eabm3108.

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