1. Epigenetics
  2. Histone Demethylase
  3. CBB1007

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.

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CBB1007

CBB1007 Chemical Structure

CAS No. : 1379573-92-8

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Top Publications Citing Use of Products

1 Publications Citing Use of MCE CBB1007

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    CBB1007 purchased from MedChemExpress. 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 .

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    Description

    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)

    In Vitro

    CBB1007 (0-100 μM; 30 h; F9) inhibits F9 cell growth[2].
    CBB1007 (5-20 μM; 14 days; hESCs) increases lipid droplet formation in hESCs during adipogenesis[1].
    CBB1007 (5-20 μM; 14 days; hESCs) reduces LSD1 and histone H3 levels while increasing H3K4me2 in human embryonic stem cells (hESCs)[1].
    CBB1007 (5-20 μM; 14 days; hESCs) upregulates adipocyte marker genes PPARγ-2 and C/EBPα in hESCs[1].
    CBB1007 (0.5-20 μM; 24 h; F9) activates the expression of CHRM4 and SCN3A genes[2].
    CBB1007 (10 μM) significantly blocks the demethylase activity of LSD1 on mono- and di-methylated H3K4, but not tri-methylated H3K4 or di-methylated H3K9[2].

    MedChemExpress (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.
    Molecular Weight

    534.61

    Formula

    C27H34N8O4

    CAS No.
    SMILES

    NC(N1CCN(CC1)CC2=CC(C(OC)=O)=CC(C(N3CCN(CC3)C(C4=CC=C(C=C4)C(N)=N)=O)=O)=C2)=N

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

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

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    • 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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    Product Name:
    CBB1007
    Cat. No.:
    HY-15313
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