APS-2-79

  • 化学数据
CAS号 2002381-25-9 货号 BCP24938
中文名 APS-2-79
英文名 APS-2-79
中文别名
英文别名 APS 2-79; APS2-79; APS-279; APS 279; APS279;
分子式 C23H21N3O3 分子量 387.43
  • 用途
生物活性 APS-2-79 is a KSR-dependent MAPK modulator. APS-2-79 modulates KSR-dependent MAPK signalling by antagonizing RAF heterodimerization as well as the conformational changes required for phosphorylation and activation of KSR-bound MEK (mitogen-activated protein kinase kinase). APS-2-79 increased the potency of several MEK inhibitors specifically within Ras-mutant cell lines by antagonizing release of negative feedback signalling, demonstrating the potential of targeting KSR to improve the efficacy of current MAPK inhibitors. Co-targeting of enzymatic and scaffolding activities within Ras-MAPK signalling complexes is a therapeutic strategy for overcoming Ras-driven cancers.
信号通路 MAPK Pathway 
靶 点 MEK/ERK 

结构式

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