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GNA002

Chemical Structure : GNA002

CAS No.: 1385035-79-9

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GNA002 (GNA-002)

Catalog No.: PC-35431Not For Human Use, Lab Use Only.

GNA002 (GNA-002) is a gambogenic acid (GNA) derivative that specifically and covalently binds to Cys668 within the EZH2-SET domain, trigges EZH2 degradation (IC50=1.1 uM) through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    GNA002 (GNA-002) is a gambogenic acid (GNA) derivative that specifically and covalently binds to Cys668 within the EZH2-SET domain, trigges EZH2 degradation (IC50=1.1 uM) through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination.
    GNA002 is a relatively more potent EZH2 interacting agent than GNA, significantly suppresses H3K27Me3 and effectively reactivated PRC2-silenced tumor suppressor genes.

    Physicochemical Properties

    M.Wt 701.901
    Formula C42H55NO8
    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

    (Z)-4-((1S,3aR,5S,12aS)-9-((E)-3,7-dimethylocta-2,6-dien-1-yl)-8,10-dihydroxy-2,2-dimethyl-11-(3-methylbut-2-en-1-yl)-4,7-dioxo-1,2,5,7-tetrahydro-1,5-methanofuro[2,3-d]xanthen-3a(4H)-yl)-N-(2-ethoxyethyl)-2-methylbut-2-enamide

    References

    1. Wang X, et al. EMBO J. 2017 May 2;36(9):1243-1260.

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