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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Aldose Reductase-Pan-AKR1C inhibitor 29
Pan-AKR1C inhibitor 29

Chemical Structure : Pan-AKR1C inhibitor 29

CAS No.:

Pan-AKR1C inhibitor 29

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 405.47
分子式 C22H19N3O3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
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

参考文献

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

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