APS-2-79
| CAS No. | 2002381-25-9 | Cat. No. | BCP24938 |
| Name | APS-2-79 | ||
| Synonyms | APS 2-79; APS2-79; APS-279; APS 279; APS279; | ||
| Formula | C23H21N3O3 | M. Wt | 387.43 |
| Description | 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. | ||
| Pathways | MAPK Pathway | ||
| Targets | MEK/ERK | ||
Structure
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