1. Epigenetics
  2. Histone Demethylase
  3. CBB1007

CBB1007 是一种可逆、选择性的 LSD1 抑制剂,对人 LSD1 的 IC50 为 5.27 µM。CBB1007 可显著抑制 LSD1 对 H3K4Me2 和 H3K4Me 的去甲基化酶活性。CBB1007 对 LSD1 的选择性高于 LSD2 或 JARID1A,并可诱导多能细胞中的分化相关基因。CBB1007 目前已在非多能性癌症研究中开展研究,靶向畸胎癌、胚胎癌和精原瘤。

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CBB1007

CBB1007 Chemical Structure

CAS No. : 1379573-92-8

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MCE 顾客使用本产品发表的 1 篇科研文献

WB

    CBB1007 purchased from MCE. Usage Cited in: BMC Neurosci. 2022 Nov 10;23(1):63.  [Abstract]

    CBB1007 (CBB) elevates H3K4me2 expression in RGC-5 cells, after which miR-21-5p expression levels are increased .

    查看 Histone Demethylase 亚型特异性产品:

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    CBB1007 is a reversible and selective LSD1 inhibitor with an IC50 of 5.27 µM for human LSD1. CBB1007 significantly blocks the demethylase activity of LSD1 on H3K4Me2 and H3K4Me. CBB1007 shows selectivity for LSD1 over LSD2 or JARID1A, and induces differentiation-related genes in pluripotent cells. CBB1007 is studied in non-pluripotent cancer research, targeting teratocarcinoma, embryonic carcinoma, and seminoma[1][2].

    IC50 & Target[2]

    KDM1/LSD1

    5.27 μM (IC50)

    体外研究
    (In Vitro)

    CBB1007(0-100 μM;30 小时;F9) 抑制 F9 细胞生长[2]
    CBB1007 (5-20 μM;;14 天;hESCs) 在脂肪分化过程中增加 hESCs 中的脂滴形成[1]
    CBB1007 (5-20 μM;14 天;hESCs) 可降低人胚胎干细胞 (hESC) 中的 LSD1 和组蛋白 H3 水平,同时增加 H3K4me2 水平[1]
    CBB1007 (5-20 μM;14 天;hESC) 可上调 hESC 中的脂肪细胞标志基因 PPARγ-2 和 C/EBPα[1]
    CBB1007 (0.5-20 μM;24 小时;F9) 激活 CHRM4 和 SCN3A 基因的表达[1]
    CBB1007 (10 μM) 可显著抑制 LSD1 对单甲基化和二甲基化 H3K4 的去甲基化酶活性,但对三甲基化 H3K4 或二甲基化 H3K9 的去甲基化酶活性无效[2]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Proliferation Assay[2]

    Cell Line: F9 cell
    Concentration: 1 μM, 5 μM, 10 μM, 50 μM, 100 μM
    Incubation Time: 30 h
    Result: Cell growth was significantly inhibited.

    Cell Differentiation Assay[1]

    Cell Line: hESCs
    Concentration: 5 μM, 10 μM, 20 μM
    Incubation Time: 14 days
    Result: LSD1 and histone H3 expression decreased, while H3K4me2 levels increased with higher doses.

    Western Blot Analysis[1]

    Cell Line: hESCs
    Concentration: 5 μM, 10 μM, 20 μM
    Incubation Time: 14 days
    Result: LSD1 and histone H3 expression decreased, while H3K4me2 levels increased with higher doses.

    RT-PCR[1]

    Cell Line: hESCs
    Concentration: 5 μM, 10 μM, 20 μM
    Incubation Time: 14 days
    Result: PPARγ-2 and C/EBPα expression increased with increasing doses.

    RT-PCR[2]

    Cell Line: F9 cell
    Concentration: 0.5 μM, 1 μM, 5 μM, 20 μM
    Incubation Time: 24 h
    Result: The expression of CHRM4 and SCN3A genes were activated. And markedly induced the expression of genes for differentiation, such as FOXA2.
    分子量

    534.61

    Formula

    C27H34N8O4

    CAS 号
    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.

    纯度 & 产品资料
    参考文献
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    产品名称:
    CBB1007
    目录号:
    HY-15313
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