AKR1B10-IN-1

• 常用名: AKR1B10-IN-1
• 英文名: AKR1B10-IN-1
• CAS号: 2136579-33-2
• 分子量: 341.33
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₉H₁₆FNO₄
• 熔点: N/A
• 闪点: N/A

AKR1B10-IN-1用途

AKR1B10-IN-1是AKR1B10(醛酮还原酶1B10)的有效抑制剂,IC50为3.5 nM。AKR1B10-IN-1抑制肺癌细胞的增殖、转移和顺铂(CDDP)耐药性[1]。

AKR1B10-IN-1名称

• 英文名: AKR1B10-IN-1

AKR1B10-IN-1生物活性

• 描述: AKR1B10-IN-1是AKR1B10(醛酮还原酶1B10)的有效抑制剂,IC50为3.5 nM。AKR1B10-IN-1抑制肺癌细胞的增殖、转移和顺铂(CDDP)耐药性[1]。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 代谢酶/蛋白酶 >> 醛糖还原酶
• 靶点实验:

  3.5 nM (AKR1B10); 277 nM (AKR1B1)[1]

• 体外研究: AKR1B10-IN-1(化合物4e)(0-20μM；96小时)剂量依赖性地抑制A549和A549/1B10细胞的生长[1]。AKR1B10-IN-1(化合物4e)(0-20μM；96小时)通过过度表达AKR1B10以及内源性蛋白完全抑制细胞增殖增加[1]。AKR1B10-IN-1(化合物4e)(0-40μM；26小时；用AKR1B10-IN-1预处理2小时,然后与CDDP孵育24小时)以剂量依赖性方式降低CDDP-R-A549细胞的细胞活力[1]。细胞活力测定[1]细胞系：A549细胞,A549/1B10细胞(AKR1B10稳定过度表达A549细胞)浓度：0,10,20 μM培养时间：96小时结果：剂量依赖性地抑制A549和A549/1B10细胞的生长,在20μM时具有统计学意义。细胞活力测定[1]细胞系：A549细胞的CDDP抗性(顺铂抗性)浓度：0,10,20,40 μM孵育时间：用AKR1B10-IN-1预处理2小时,然后用CDDP孵育24小时结果：CDDP-R-A549细胞的存活率呈剂量依赖性降低,40μM处理最为明显。
• 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.

AKR1B10-IN-1物理化学性质

• 分子式: C₁₉H₁₆FNO₄
• 分子量: 341.33

AKR1B10-IN-1靶点实验

查看更多实验

实验名称：Antimigratory activity in human A549-Luc2 cells xenografted in C.B-17/IcrHsd-Prkdcsci... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4020455

实验名称：Antiproliferative activity against human A549/CDDP cells assessed as decrease in cell... 来源：ChEMBL 靶标：A549/CDDP External Id：CHEMBL4020456

实验名称：Antiproliferative activity against human A549 cells after 96 hrs by tetrazolium-dye b... 来源：ChEMBL 靶标：A549 External Id：CHEMBL4020453

实验名称：Antiproliferative activity against human A549/1B10 cells after 96 hrs by tetrazolium-... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4020454

实验名称：Antimigratory activity in human A549 cells at 20 uM after 24 hrs by wound-healing ass... 来源：ChEMBL 靶标：A549 External Id：CHEMBL4020452

实验名称：Selectivity ratio of IC50 for recombinant human AKR1B1 to IC50 for recombinant human ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4020430

实验名称：Antiinvasive activity in human A549/CDDP cells at 10 to 20 uM after 48 hrs by boyden ... 来源：ChEMBL 靶标：A549/CDDP External Id：CHEMBL4020459

实验名称：Inhibition of recombinant human AKR1B10 using pyridine-3-aldehyde as substrate 来源：ChEMBL 靶标：Aldo-keto reductase family 1 member B10 External Id：CHEMBL4020427

实验名称：Inhibition of recombinant human AKR1B1 using pyridine-3-aldehyde as substrate 来源：ChEMBL 靶标：Aldo-keto reductase family 1 member B1 External Id：CHEMBL4020428

实验名称：Antiproliferative activity against human A549/CDDP cells assessed as decrease in cell... 来源：ChEMBL 靶标：A549/CDDP External Id：CHEMBL4020457

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AKR1B10-IN-1英文别名

• N-(3-(4-Fluorophenyl)propyl) -7-hydroxycoumarin-3-carboxamide