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首页-小分子抑制剂&激动剂-Wnt/Notch/Hedgehog-Beta-catenin-E722-2648
E722-2648

Chemical Structure : E722-2648

CAS No.: 931963-55-2

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

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    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.

    物理化学性质&存储条件

    分子量 390.604
    分子式 C21H30N2OS2
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    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

    参考文献

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

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