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CAS No. | 2002381-25-9 | Cat. No. | BCP24938 |
Name | APS-2-79 | ||
Synonyms | APS 2-79; APS2-79; APS-279; APS 279; APS279; | ||
SMILES | CC1=C(C=CC(=C1)OC2=CC=CC=C2)NC3=NC=NC4=CC(=C(C=C43)OC)OC | ||
Chemical Name | |||
Formula | C23H21N3O3 | M. Wt | 387.43 |
Purity | 98% | Storage | Store at 4-8°C |
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. |
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