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Pan-AKR1C inhibitor 29

Chemical Structure : Pan-AKR1C inhibitor 29

CAS No.: 3114057-78-9

Pan-AKR1C inhibitor 29

Catalog No.: PC-24206Not For Human Use, Lab Use Only.

Pan-AKR1C inhibitor 29 is a potent, pan-AKR1C (aldo-keto reductase family 1 member C) inhibitor with IC50 of 0.09 μM, 0.28 μM, 0.05 μM, 0.51 μM for AKR1C1, AKR1C2, AKR1C3, and AKR1C4 respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    Pan-AKR1C inhibitor 29 is a potent, pan-AKR1C (aldo-keto reductase family 1 member C) inhibitor with IC50 of 0.09 μM, 0.28 μM, 0.05 μM, 0.51 μM for AKR1C1, AKR1C2, AKR1C3, and AKR1C4 respectively.
    Pan-AKR1C inhibitor 29 significantly induced the anti-proliferative effect of DOX on MCF-7/ADR.
    Pan-AKR1C inhibitor 29 exhibited synergistic effects, as evidenced by the calculated CI values (0.221–0.524) within the synergistic range for MCF-7/ADR cells, when combined with DOX.
    The combination of 29 with DOX effectively suppressed cell proliferation and reversed DOX resistance.
    Pan-AKR1C inhibitor 29 can enhance DOX-induced DNA damage, thereby inducing apoptosis and ultimately reversing DOX-resistance.
    Pan-AKR1C inhibitor 29 significantly sensitized DOX-resistance cancer cells to DOX on MCF-7/ADR xenograft models.

    Physicochemical Properties

    M.Wt 405.47
    Formula C22H19N3O3S
    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

    7-(2-((6-oxo-4-phenyl-1,6-dihydropyrimidin-2-yl)thio)acetyl)-1,3,4,5-tetrahydro-2H-benzo[b]azepin-2-one

    References

    1. Xing S, et al. Eur J Med Chem. 2025 Feb 20;289:117413.

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