Chemical Structure : Pan-AKR1C inhibitor 29
CAS No.:
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)
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
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M.Wt
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405.47
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Formula
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C22H19N3O3S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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7-(2-((6-oxo-4-phenyl-1,6-dihydropyrimidin-2-yl)thio)acetyl)-1,3,4,5-tetrahydro-2H-benzo[b]azepin-2-one
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References
1. Xing S, et al. Eur J Med Chem. 2025 Feb 20;289:117413.
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