AKR1B10-IN-1

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

AKR1B10-IN-1 

AKR1B10-IN-1 是一种有效的 AKR1B10 抑制剂，IC50 值为 3.5 nM。AKR1B10-IN-1 抑制顺铂 (Cisplatin) 耐药的肺癌细胞的增殖和转移。

AKR1B10-IN-1

AKR1B10-IN-1 Chemical Structure

CAS No. : 2136579-33-2

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生物活性

AKR1B10-IN-1 is a potent inhibitor of AKR1B10 (Aldo-Keto Reductase 1B10) with an IC50 of 3.5 nM. AKR1B10-IN-1 suppresses proliferation, metastasis, and Cisplatin (CDDP) resistance of lung cancer cells[1].

IC50 & Target

3.5 nM (AKR1B10); 277 nM (AKR1B1)[1]
体外研究
(In Vitro)

AKR1B10-IN-1 (compound 4e) (0-20 μM; 96 hours) dose-dependently suppresses the growth of both A549 and A549/1B10 cells[1].
AKR1B10-IN-1 (compound 4e) (0-20 μM; 96 hours) completely suppresses increased cell proliferation by the overexpressing AKR1B10 as well as the endogenous protein[1].
AKR1B10-IN-1 (compound 4e) (0-40 μM; 26 hours; pretreatment with AKR1B10-IN-1 for 2 hours, then incubated with CDDP for 24 hours) decreases the cell viability of CDDP-R-A549 cells in a dose-dependent manner[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: A549 cells, A549/1B10 cells (AKR1B10-stably overexpressing A549 cells)
Concentration: 0, 10, 20 μM
Incubation Time: 96 hours
Result: Dose-dependently suppressed the growth of both A549 and A549/1B10 cells, and statistically significant at 20 μM.

Cell Viability Assay[1]

Cell Line: CDDP-resistance (cisplatin-resisitance) of A549 cells
Concentration: 0, 10, 20, 40 μM
Incubation Time: Pretreatment with AKR1B10-IN-1 for 2 hours, then incubated with CDDP for 24 hours
Result: Decreased the cell viability of CDDP-R-A549 cells in a dose-dependent manner, and most obvious in the treatment of 40 μM.

分子量

341.33

Formula

C19H16FNO4
CAS 号

2136579-33-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Endo S, et al. Synthesis of Potent and Selective Inhibitors of Aldo-Keto Reductase 1B10 and Their Efficacy against Proliferation, Metastasis, and Cisplatin Resistance of Lung Cancer Cells [published correction appears in J Med Chem. 2018 Feb 8;61(3):1380]. J Med Chem. 2017;60(20):8441-8455.

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