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GDCNF-11

Chemical Structure : GDCNF-11

CAS No.: 2991588-80-6

GDCNF-11 (GDCNF11)

Catalog No.: PC-26133Not For Human Use, Lab Use Only.

GDCNF-11 is a potent HSP90 interactome-mediated proteolysis targeting chimera (HIM-PROTAC) GPX4 degarder, potently induces ferroptosis via HSP90-mediated ubiquitin-proteasomal degradation of GPX4 in HT-1080 cells with DC50 of 0.08 uM.

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    Biological Activity

    GDCNF-11 is a potent HSP90 interactome-mediated proteolysis targeting chimera (HIM-PROTAC) GPX4 degarder, potently induces ferroptosis via HSP90-mediated ubiquitin-proteasomal degradation of GPX4 in HT-1080 cells with DC50 of 0.08 uM.
    GDCNF-11 showed 15-fold more ferroptosis selectivity over GPX4 inhibitor ML162.
    GDCNF-11 effectively suppress tumor growth in the mice model with relatively low toxicity as compared to the combination therapy of GPX4 and HSP90 inhibitors.

    Physicochemical Properties

    M.Wt 995.00
    Formula C48H53Cl2N13O5S
    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-Thiopheneacetamide, α-[[4-[[1-[2-[4-[2-[[2-amino-9-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]-9H-purin-6-yl]amino]ethyl]-1-piperidinyl]-2-oxoethyl]-1H-1,2,3-triazol-4-yl]methoxy]-3-chlorophenyl](2-chloroacetyl)amino]-N-(2-phenylethyl)-

    References

    1. Jinyun Dong, et al. J Med Chem. 2024 Sep 26;67(18):16712-16736.

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