APS-2-79 HCl

Description: APS-2-79 HCl, the hydrochloride salt of APS-2-79, is an antagonist of MAPK (mitogen-activated protein kinase) that modulates KSR-dependent MAPK signalling by antagonizing RAF heterodimerization as well as the conformational changes required for phosphorylation and activation of KSR-bound MEK. APS-2-79 was found to be able to suppress KSR-stimulated MEK and ERK phosphorylation. This MAPK signalling suppression caused by APS-2-79 was dependent on direct targeting of KSR as an active site mutant, which had been demonstrated to stimulate KSR-based MAPK outputs independent of ATP-binding, which could significantly diminish the activity of APS-2-79. Moreover, the KSR-stimulated MEK phosphorylation caused by RAF was reduced by the addition of APS-2-79 markedly. APS-2-79 has the potential to improve the efficacy of current MAPK inhibitors and may be used as a therapeutic strategy for Ras-driven cancers.

References: Nature. 2016 Sep 1; 537(7618):112-116.

Related CAS#:2002381-25-9 (free base)