APS-2-79
| 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 |
| 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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