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3JC48-3

Chemical Structure : 3JC48-3

CAS No.: 1629989-75-8

3JC48-3 (3jc48-3)

Catalog No.: PC-38435Not For Human Use, Lab Use Only.

3JC48-3 is a potent, cellularly active and stable c-Myc inhibitor, inhibits c-Myc-max dimerization with IC50 of 34 uM, 5 times more potent than 10074-G5, exhibits an approximate twofold selectivity for c-Myc-Max heterodimers over Max-Max homodimers.

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    Biological Activity

    3JC48-3 is a potent, cellularly active and stable c-Myc inhibitor, inhibits c-Myc-max dimerization with IC50 of 34 uM, 5 times more potent than 10074-G5, exhibits an approximate twofold selectivity for c-Myc-Max heterodimers over Max-Max homodimers.
    3JC48-3 inhibited the proliferation of c-Myc-over-expressing HL60 and Daudi cells with single-digit micromolar IC50 values by causing growth arrest at the G0 /G1 phase.
    3JC48-3 inhibited c-Myc-Max dimerization in cells validated by CoIP.
    3JC48-3 decreased prostate cancer cells' growth and viability in a dose-dependent fashion in vitro, upregulated PrKD1 expression and phosphorylation of known PrKD1 substrates: the threonine 120 (Thr-120) residue in beta-catenin and the serine 216 (Ser-216) in Cell Division Cycle 25 (CDC25C).
    3JC48-3 (100 mg/kg, i.p.) decreased the rate of tumor growth in mice with patient-derived prostate cancer xenografts (PDX), without dose-limiting toxicity.

    Physicochemical Properties

    M.Wt 404.382
    Formula C21H16N4O5
    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

    methyl 4'-methyl-6-((7-nitrobenzo[c][1,2,5]oxadiazol-4-yl)amino)-[1,1'-biphenyl]-3-carboxylate

    References

    1. Chauhan J, et al. ChemMedChem. 2014 Oct;9(10):2274-2285.

    2. Shukla S, et al. Cancer Gene Ther. 2022 Apr 19. doi: 10.1038/s41417-022-00455-4.

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