mao a/hsp90-in-1

MAO A/HSP90-IN-1 (4-b) is a dual inhibitor of MAO A and HSP90, with IC50 values of 1.77 μM in glioblastoma (GBM) GL26 cells and 0.019 μM against HSP90α. This compound impairs MAO A activity, disrupts HSP90 binding, and downregulates HER2 and phospho-Akt expressions, thus inhibiting GBM growth. Additionally, it reduces PD-L1 expression, thwarting T cell activation and potential tumor immune evasion. MAO A/HSP90-IN-1 (4-b) is valuable for research into brain tumor-related diseases [1].

MAO A/HSP90-IN-2 (compound 4-C), a dual inhibitor of HSP90 and MAO A, exhibits IC50 values of 0.016 μM for MAO A and 4.58 μM for HSP90. This compound enhances HSP70 expression, diminishes HER2 and phospho-Akt levels, downregulates IFN-γ-induced PD-L1 expression in GL26 cells, and demonstrates efficacy against Temozolomide-sensitive and -resistant GBM cells, colon cancer, leukemia, and non-small cell lung cancer, possibly impeding tumor immune evasion [1].