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AG-1031

Chemical Structure : AG-1031

CAS No.:

AG-1031 (AG1031)

Catalog No.: PC-20734Not For Human Use, Lab Use Only.

AG-1031 (AG1031) is a specific small molecule inhibitor of the double-stranded DNA binding activity of positive coactivator 4 (PC4) with IC50 of 2.5 uM, more effectively than its single-stranded DNA binding activity (IC50=15 uM).

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    Biological Activity

    AG-1031 (AG1031) is a specific small molecule inhibitor of the double-stranded DNA binding activity of positive coactivator 4 (PC4) with IC50 of 2.5 uM, more effectively than its single-stranded DNA binding activity (IC50=15 uM).
    AG-1031 specifically inhibited PC4-dependent transcriptional activation in vitro using purified transcription factors.
    AG-1031 also interfered with PC4 binding to a monoclonal antibody against PC4 and with PC4 binding to the transcription activator VP16.
    AG-1031 (0.3 μM, 72 h) inhibited the viability of lung adenocarcinoma cell line A549 cells, significantly reduced the expression of PC4.
    AG-1031 (40 μg/mouse) inhibited tumor growth in A549 cell xenografts, with reduced level of PC4 protein.
    AG-1031 induced autophagic cell death and apoptosis in C6 glioma cells associated with Notch-1 signaling pathway.

    Physicochemical Properties

    M.Wt 718.8
    Formula C41H42N4O8
    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

    (4R,4aS)-18-Ethenyl-4,4a-dihydro-3,4-bis(methoxycarbonyl)-4a,8,14,19-tetramethyl-24H,26H-benzo[b]porphine-9,13-dipropanoic acid monomethyl ester

    References

    1. Wang Y, et al. J Cell Biochem. 2018 Jul;119(7):5893-5903.

    2. Zhang Y,et al. PLoS One. 2020 Mar 31;15(3):e0230670.

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