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KDOBA67

Chemical Structure : KDOBA67

CAS No.:

KDOBA67 (KDOBA 67)

Catalog No.: PC-72453Not For Human Use, Lab Use Only.

KDOBA67 is a novel cell-permeable inhibitor of H3K27 lysine demethylase KDM6A/B, inhibits TBXT expression chordoma cell lines.

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    Biological Activity

    KDOBA67 is a novel cell-permeable inhibitor of H3K27 lysine demethylase KDM6A/B, inhibits TBXT expression chordoma cell lines.
    KDOBA67 displayed in vitro inhibitory activity in the low micromolar range with IC50 values of 2 to 5 uM in various chordoma cell lines, leading to induction of apoptosis.
    H3K27 demethylase inhibition via KDOBA67 alters chromatin state at TBXT and inhibits its expression.
    TBXT was a KDM6A/B target gene, and chromatin changes at TBXT following KDOBA67 treatment were associated with a reduction in TBXT protein levels.
    KDOBA67 treatment downregulated expression of a network of transcription factors critical for chordoma survival and upregulated pathways dominated by ATF4-driven stress and proapoptotic responses.

    Physicochemical Properties

    M.Wt 361.449
    Formula C21H23N5O
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    2-((2-(pyridin-3-yl)-6-(1,2,4,5-tetrahydro-3H-benzo[d]azepin-3-yl)pyrimidin-4-yl)amino)ethan-1-ol

    References

    1. Lucia Cottone, et al. Cancer Res. 2020 Oct 15;80(20):4540-4551.

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