APS-2-79

APS-2-79 is a small molecule inhibitor of the pseudokinase and scaffold protein Kinase Suppressor of Ras 2 (KSR2). It was originally developed as a tool compound to probe the KSR-MEK interaction, binding to the ATP-binding site of KSR to induce a conformational change that prevents the recruitment and activation of MEK by Raf. In the context of oncology, particularly the TAL1 molecular subtype of T-cell acute lymphoblastic leukemia (T-ALL), APS-2-79 has been shown to decrease cell viability and proliferation by disrupting KSR2-mediated signaling pathways, including AMPK signaling, which is critical for leukemic cell survival. While primarily utilized as a research-use-only reagent, its efficacy in preclinical models suggests potential for development as a targeted therapy for high-risk pediatric leukemia patients exhibiting ectopic KSR2 expression.