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EPIC-0412

Chemical Structure : EPIC-0412

CAS No.: 3034959-62-8

EPIC-0412 (EPIC0412)

Catalog No.: PC-49393Not For Human Use, Lab Use Only.

EPIC-0412 is a small-molecule inhibitor that enhances the chemotherapeutic effect of temozolomide (TMZ) by acting on the p21-E2F1 DNA damage repair axis and ATF3-p-p65-MGMT axis.

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    Biological Activity

    EPIC-0412 is a small-molecule inhibitor that enhances the chemotherapeutic effect of temozolomide (TMZ) by acting on the p21-E2F1 DNA damage repair axis and ATF3-p-p65-MGMT axis.
    EPIC-0412 physically interrupts the binding of HOTAIR and EZH2, leading to the upregulation of CDKN1A and BBC3, causing cell cycle arrest and apoptosis in GBM cells.
    EPIC-0412 inhibits DNA damage response in GBM cells through the p21-E2F1 DNA damage repair axis.
    EPIC-0412 epigenetically silences MGMT through its interaction with the ATF3-p-p65-HADC1 axis at the MGMT promoter region.
    EPIC-0412 restored the TMZ sensitivity in GBM in vivo experiments.

    Physicochemical Properties

    M.Wt 423.387
    Formula C21H18F5N3O
    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

    1-(3-((2,4-difluorobenzyl)oxy)benzyl)-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine

    References

    1. Zhao J, et al. Neuro Oncol. 2022 Oct 22:noac242.

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