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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-AC1Q3QWB
AC1Q3QWB

Chemical Structure : AC1Q3QWB

CAS No.: 46697-00-1

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AC1Q3QWB (AQB)

货号: PC-26182Not For Human Use, Lab Use Only.

AC1Q3QWB (AQB) is a selective and efficient inhibitor of HOTAIR-EZH2 interaction with IC50 of 42.47 nM, exhibits potent anti-tumor activity in cancer cells expressing high levels of HOTAIR and EZH2.

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

    生物&药学活性

    AC1Q3QWB (AQB) is a selective and efficient inhibitor of HOTAIR-EZH2 interaction with IC50 of 42.47 nM, exhibits potent anti-tumor activity in cancer cells expressing high levels of HOTAIR and EZH2.
    ACB selectively blocks HOTAIR-EZH2 interaction and reduces recruitment of PRC2, does not affect EZH2-binding lincRNAs, including GTL2 10, and H19, also does not affect HOTAIR-chromatin interaction.
    AQB can effectively up-regulate both mRNA and protein levels of HOTAIR-PRC2 target genes, suppresses Wnt/β-catenin signaling by upregulating APC2 expression.
    AQB (50mg/kg) inhibits tumor growth and metastasis in MDA-MB-231 orthotopic breast cancer model, inhibits tumor cell growth and metastasis in vivo.
    Low doses of AQB enhance the efficacy of DZNep resulting from more significant expression of HOTAIR-PRC2 target genes.

    物理化学性质&存储条件

    分子量 260.16
    分子式 C12H15Cl2NO
    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-((5,7-dichloro-2,3-dihydrobenzofuran-2-yl)methyl)propan-2-amine

    参考文献

    1. Li Y, et al. Theranostics. 2019 Jun 24;9(16):4608-4623.

    2. Shi J, et al. Clin Transl Med. 2020 Jan;10(1):182-198.

    3. Tong F, et al. Pharmacol Res. 2023 Jan;187:106606.

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