首页 产品中心
  • CBB1007 trihydrochloride
    • CBB1007 3HCl
    货号: abs818690
    CAS号: 1379573-92-8(free base)
    分子式: C27H37Cl3N8O4
    分子量: 643.99
    产品说明书
    分享:
    货号-规格 货期 价格 数量
    abs818690-2mg 1-2周 ¥3077.00
    - +
    abs818690-5mg 1-2周 ¥4614.00
    - +
    大包装询价
    产品描述
    描述

    CBB1007 trihydrochloride is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1).

    储存/保存方法
    Store at -20°C
    基本信息
    别名
    CBB1007 3HCl
    可溶性/溶解性
    DMSO : ≥ 54 mg/mL (83.85 mM)
    参考文献
    参考文献
    [1]. Wang J, et al. Novel histone demethylase LSD1 inhibitors selectively target cancer cells with pluripotent stem cell properties. Cancer Res. 2011 Dec 1;71(23):7238-49.

    Abstract

    Histone modification determines epigenetic patterns of gene expression with methylation of histone H3 at lysine 4 (H3K4) often associated with active promoters. LSD1/KDM1 is a histone demethylase that suppresses gene expression by converting dimethylated H3K4 to mono- and unmethylated H3K4. LSD1 is essential for metazoan development, but its pathophysiologic functions in cancer remain mainly uncharacterized. In this study, we developed specific bioactive small inhibitors of LSD1 that enhance H3K4 methylation and derepress epigenetically suppressed genes in vivo. Strikingly, these compounds inhibited the proliferation of pluripotent cancer cells including teratocarcinoma, embryonic carcinoma, and seminoma or embryonic stem cells that express the stem cell markers Oct4 and Sox2 while displaying minimum growth-inhibitory effects on non-pluripotent cancer or normal somatic cells. RNA interference-mediated knockdown of LSD1 expression phenocopied these effects, confirming the specificity of small molecules and further establishing the high degree of sensitivity and selectivity of pluripotent cancer cells to LSD1 ablation. In support of these results, we found that LSD1 protein level is highly elevated in pluripotent cancer cells and in human testicular seminoma tissues that express Oct4. Using these novel chemical inhibitors as probes, our findings establish LSD1 and histone H3K4 methylation as essential cancer-selective epigenetic targets in cancer cells that have pluripotent stem cell properties.
    温馨提示:本产品仅作科研实验使用,不支持临床等研究
        提示: 尊敬的客户您好,如果您对我们的产品有什么疑问或想要了解的,可以点击“我要提问”按钮填写您的疑问。
        提交不成功?请联系info@absin.cn。
        我要提问

    促销资讯 更多

      订购信息
      您可以从我们的授权经销商处购买absin产品或获得技术支持。若要查看您所在地区的经销商,请从以下的下拉列表中选择。
      GO
      • 0