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首页-小分子抑制剂&激动剂-Apoptosis-Bcl-2-BAU-243
BAU-243

Chemical Structure : BAU-243

CAS No.: 496767-27-2

BAU-243 (BAU243, AN-698/40780701)

货号: PC-20689Not For Human Use, Lab Use Only.

BAU-243 (BAU243) is a novel BH3 mimetic Bcl-2 inhibitor with a high affinity, effectively reduces overall GBM cell proliferation including a subpopulation of cancer-initiating cells.

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

    生物&药学活性

    BAU-243 (BAU243) is a novel BH3 mimetic Bcl-2 inhibitor with a high affinity, effectively reduces overall GBM cell proliferation including a subpopulation of cancer-initiating cells.
    BAU-243 reduces survival of GBM cells and tumor-initiating stem cells (A172 cells, IC50=18.2 uM).
    BAU-243 induces limited apoptosis and cell cycle arrest in low Bcl-2 expressing cells.
    BAU-243 does not induce apoptosis in high Bcl-2 expressing SHSY-5Y cells despite the significant anti-proliferative effect.
    BAU-243 promotes autophagic cell death through the disruption of Beclin 1 and Bcl-2 interaction, regardless of Bcl-2 expression level.
    BAU-243 (25 mg/kg) reduced tumor growth in vivo with lower dose compared to other BH3 mimetics (ABT-263, 75 mg/kg).
    BAU-243 demonstrated a remarkable anti-proliferative effect on the cancer sub-population that is considered a true representative of tumor-initiating GBM stem-like cells.
    BAU-243 interacts with critical residues of Bcl-2 that plays role in the binding of Beclin 1 BH3 domain, showing that it can hinder Beclin 1:Bcl-2 complex formation, freeing Beclin 1 to activate the autophagy pathway.

    物理化学性质&存储条件

    分子量 501.60
    分子式 C28H27N3O4S
    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

    2-(4-((Z)-((Z)-3-(2-methoxyethyl)-4-oxo-2-(phenylimino)thiazolidin-5-ylidene)methyl)phenoxy)-N-(p-tolyl)acetamide

    参考文献

    1. Calis S, et al. Cell Death Discov. 2022 Oct 29;8(1):433.

    2. Tutumlu G, et al. Front Chem. 2020;8.

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