LJI308

• 常用名: LJI308
• 英文名: LJI308
• CAS号: 1627709-94-7
• 分子量: 368.377
• 密度: 1.3±0.1 g/cm3
• 沸点: 486.6±45.0 °C at 760 mmHg
• 分子式: C₂₁H₁₈F₂N₂O₂
• 熔点: N/A
• 闪点: 248.1±28.7 °C

LJI308用途

LJI308是新型有效的RSK抑制剂, 抑制RSK1, RSK2, 和RSK3 IC50值分别为6 nM, 4 nM, 和13 nM。

LJI308名称

• 中文名: LJI308
• 英文名: 2,6-Difluoro-4-{4-[4-(4-morpholinyl)phenyl]-3-pyridinyl}phenol

LJI308生物活性

• 描述: LJI308是新型有效的RSK抑制剂, 抑制RSK1, RSK2, 和RSK3 IC50值分别为6 nM, 4 nM, 和13 nM。
• 相关类别:
  信号通路 >> MAPK/ERK信号通路 >> 核糖体S6激酶(RSK)
  研究领域 >> 癌症
• 参考文献:

  [1]. Aronchik I, et al. Novel potent and selective inhibitors of p90 ribosomal S6 kinase reveal the heterogeneity of RSK function in MAPK-driven cancers. Mol Cancer Res. 2014 May;12(5):803-12.

  [2]. Davies AH, et al. Inhibition of RSK with the novel small-molecule inhibitor LJI308 overcomes chemoresistance by eliminating cancer stem cells. Oncotarget. 2015 Aug 21;6(24):20570-7.

  [3]. Jain R, et al. Discovery of Potent and Selective RSK Inhibitors as Biological Probes. J Med Chem. 2015 Sep 10;58(17):6766-83.

LJI308物理化学性质

• 密度: 1.3±0.1 g/cm3
• 沸点: 486.6±45.0 °C at 760 mmHg
• 分子式: C₂₁H₁₈F₂N₂O₂
• 分子量: 368.377
• 闪点: 248.1±28.7 °C
• 精确质量: 368.133636
• LogP: 2.87
• InChIKey: YUYJEQHNWKQNBT-UHFFFAOYSA-N
• SMILES: Oc1c(F)cc(-c2cnccc2-c2ccc(N3CCOCC3)cc2)cc1F
• 外观性状: 粉末
• 蒸汽压: 0.0±1.3 mmHg at 25°C
• 折射率: 1.602
• 储存条件: -20℃

LJI308靶点实验

查看更多实验

实验名称：Antiproliferative activity against human MOLM13 assessed as reduction in cell viabili... 来源：ChEMBL 靶标：MOLM-13 External Id：CHEMBL4622997

实验名称：Inhibition of RSK2 (unknown origin) assessed as reduction in YB1 transmembrane phosph... 来源：ChEMBL 靶标：Ribosomal protein S6 kinase alpha-3 External Id：CHEMBL4266991

实验名称：Inhibition of RSK2 (unknown origin) 来源：ChEMBL 靶标：Ribosomal protein S6 kinase alpha-3 External Id：CHEMBL4266990

实验名称：Inhibition of human recombinant Histidine-tagged RSK2 using biotin-AGAGRSRHSSYPAGT-OH... 来源：ChEMBL 靶标：Ribosomal protein S6 kinase alpha-3 External Id：CHEMBL3607765

实验名称：Inhibition of RSK2 in mouse BAF cells expressing activated FGFR assessed as reduction... 来源：ChEMBL 靶标：Ribosomal protein S6 kinase alpha-3 External Id：CHEMBL3607766

实验名称：Binding affinity to DNA-tagged PLK (unknown origin) at 10 uM by qPCR analysis 来源：ChEMBL 靶标：Serine/threonine-protein kinase PLK1 External Id：CHEMBL3607885

实验名称：Binding affinity to DNA-tagged RSK1 N-terminal kinase domain (unknown origin) assesse... 来源：ChEMBL 靶标：Ribosomal protein S6 kinase alpha-1 External Id：CHEMBL3607886

实验名称：Cytotoxicity in HEK293 cells assessed as reduction in cell viability 来源：ChEMBL 靶标：HEK293 External Id：CHEMBL4623014

实验名称：Binding affinity to DNA-tagged RSK4 N-terminal kinase domain (unknown origin) assesse... 来源：ChEMBL 靶标：Ribosomal protein S6 kinase alpha-6 External Id：CHEMBL3606280

实验名称：Binding affinity to DNA-tagged RSK2 N-terminal kinase domain (unknown origin) assesse... 来源：ChEMBL 靶标：Ribosomal protein S6 kinase alpha-3 External Id：CHEMBL3607887

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LJI308英文别名

• 2,6-Difluoro-4-{4-[4-(4-morpholinyl)phenyl]-3-pyridinyl}phenol
• LJI308
• LJI-308