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ER-400583-00

Chemical Structure : ER-400583-00

CAS No.: 1338216-76-4

ER-400583-00 (HIF-1α inhibitor)

Catalog No.: PC-20456Not For Human Use, Lab Use Only.

ER-400583-00 is a small-molecule HIF-1α inhibitor, inhibits the induction of HIF-1 reporter activity in response to hypoxia with IC50 of 7.9 nM.

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    Biological Activity

    ER-400583-00 is a small-molecule HIF-1α inhibitor, inhibits the induction of HIF-1 reporter activity in response to hypoxia with IC50 of 7.9 nM.
    ER-400583-00 suppressed the hypoxia-induced accumulation of the messenger RNAs (CA9, VEGFA, and SLC2A1) in U251 cells, without effect on the amount of HIF-1α protein present in U251 cells under normoxic conditions.
    ER-400583-00 suppressed the induction of HIF-1α protein in response to hypoxia with IC50 of 3.7 nM.
    ER-400583-00 (100 mg/kg, oral) significantly decreased mRNA levels of the HIF-1 target genes CA9, VEGFA, and SLC2A1 24 h after treatment, significantly delayed tumor growth in human U251 tumor xenografts.
    ER-400583-00 suppressed cell proliferation distal to the region of blood perfusion in U251 xenograft tumors, exhibited synergistic interaction when combined with radiation therapy.
    ER-400583-00 suppressed the accumulation of HIF-1α protein under hypoxic conditions but did not affect HIF-1α mRNA levels.

    Physicochemical Properties

    M.Wt 486.62
    Formula C32H30N4O
    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

    N-(4-(phenylethynyl)phenyl)-4-((4-(pyridin-3-ylmethyl)piperazin-1-yl)methyl)benzamide

    References

    1. Kiyoshi Okamoto, et al. Int J Mol Med. 2012 Apr;29(4):541-9.

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