AMA-37

• 常用名: AMA-37
• 英文名: AMA-37
• CAS号: 404009-46-7
• 分子量: 283.32200
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₇H₁₇NO₃
• 熔点: N/A
• 闪点: N/A

AMA-37用途

AMA-37是一种芳基吗啉类似物,是ATP竞争性DNA-PK抑制剂,IC50值分别为0.27μM(DNA-PK)、32μM(p110α)、3.7μM(p110β)和22μM(p110γ)[1][2]。

AMA-37名称

• 中文名: DNA-PK抑制剂V
• 英文名: (2-hydroxy-4-morpholin-4-ylphenyl)-phenylmethanone

AMA-37生物活性

• 描述: AMA-37是一种芳基吗啉类似物,是ATP竞争性DNA-PK抑制剂,IC50值分别为0.27μM(DNA-PK)、32μM(p110α)、3.7μM(p110β)和22μM(p110γ)[1][2]。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 细胞周期/DNA损伤 >> DNA-PK
  信号通路 >> PI3K/Akt/mTOR 信号通路 >> DNA-PK
• 靶点实验:

  IC50: 0.27 μM (DNA-PK)[1].

• 体外研究: AMA-37对PI3K的抑制作用较差[2]。AMA-37(20μM)可降低UCN-01、异肉芽酰胺和去甲海松烯醛二烯(而非咖啡因)克服G2期阻滞的能力(ρ<0.05)[3]。用AMA37抑制DNA-PK可导致放射增敏[3]。
• 参考文献:

  [1]. Zachary A Knight, et al. A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. Cell. 2006 May 19;125(4):733-47.

  [2]. Zachary A Knight, et al. Isoform-specific phosphoinositide 3-kinase inhibitors from an arylmorpholine scaffold. Bioorg Med Chem. 2004 Sep 1;12(17):4749-59.

  [3]. Christopher M Sturgeon, et al. Effect of combined DNA repair inhibition and G2 checkpoint inhibition on cell cycle progression after DNA damage. Mol Cancer Ther. 2006 Apr;5(4):885-92.

AMA-37物理化学性质

• 分子式: C₁₇H₁₇NO₃
• 分子量: 283.32200
• 精确质量: 283.12100
• PSA: 49.77000
• LogP: 2.52480
• InChIKey: FALILNHGILFDLC-UHFFFAOYSA-N
• SMILES: O=C(c1ccccc1)c1ccc(N2CCOCC2)cc1O
• 储存条件: -20℃

AMA-37靶点实验

查看更多实验

实验名称：Millipore: Percentage of residual kinase activity of PRKAA2 at 10uM relative to contr... 来源：ChEMBL 靶标：5'-AMP-activated protein kinase catalytic subunit alpha-1 External Id：CHEMBL2219380

实验名称：Millipore: Percentage of residual kinase activity of NUAK1 at 1uM relative to control... 来源：ChEMBL 靶标：NUAK family SNF1-like kinase 1 External Id：CHEMBL2219381

实验名称：Millipore: Percentage of residual kinase activity of PRKAA1 at 10uM relative to contr... 来源：ChEMBL 靶标：5'-AMP-activated protein kinase catalytic subunit alpha-1 External Id：CHEMBL2219378

实验名称：Millipore: Percentage of residual kinase activity of PRKAA2 at 1uM relative to contro... 来源：ChEMBL 靶标：5'-AMP-activated protein kinase catalytic subunit alpha-1 External Id：CHEMBL2219379

实验名称：Millipore: Percentage of residual kinase activity of MAP3K5 at 10uM relative to contr... 来源：ChEMBL 靶标：Mitogen-activated protein kinase kinase kinase 5 External Id：CHEMBL2218943

实验名称：Millipore: Percentage of residual kinase activity of ABL1 at 1uM relative to control.... 来源：ChEMBL 靶标：Tyrosine-protein kinase ABL1 External Id：CHEMBL2218944

实验名称：Millipore: Percentage of residual kinase activity of NUAK1 at 10uM relative to contro... 来源：ChEMBL 靶标：NUAK family SNF1-like kinase 1 External Id：CHEMBL2219382

实验名称：Millipore: Percentage of residual kinase activity of MAP3K5 at 1uM relative to contro... 来源：ChEMBL 靶标：Mitogen-activated protein kinase kinase kinase 5 External Id：CHEMBL2219383

实验名称：Millipore: Percentage of residual kinase activity of TNK2 at 10uM relative to control... 来源：ChEMBL 靶标：Activated CDC42 kinase 1 External Id：CHEMBL2219372

实验名称：Millipore: Percentage of residual kinase activity of ALK at 1uM relative to control. ... 来源：ChEMBL 靶标：ALK tyrosine kinase receptor External Id：CHEMBL2219373

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AMA-37英文别名

• AMA37
• ArylMorpholine Analog 37
• 1-(2-Hydroxy-4-morpholin-4-yl-phenyl)-phenyl-methanone
• DNA-PK Inhibitor V