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].

MAO-A:4.58 μM, HSP90:0.016 μM

MAO A/HSP90-IN-2 inhibits the growth of murine and human glioma cells, as well as colon cancer, leukemia, and non-small cell lung cancer cells (GL26, U251S, U251R, U87MG, U373MG, and LN229, with IC50 values of 0.49, 1.09, 0.26, 0.36, 0.89, and 0.31 μM, respectively) [1]. The compound, at concentrations of 0.3 to 3 μM for 24 hours, upregulates HSP70 expression and downregulates HER2 and phosphorylated AKT expression in GL26 and U251R cells [1]. Additionally, MAO A/HSP90-IN-2, at doses of 0.5 to 1 μM over 24 hours, suppresses the IFN-γ-induced upregulation of PD-L1 in GL26 cells [1].

MAO A/HSP90-IN-2 (Compound 4-C) administered at a dose of 25mg/kg via intraperitoneal injection for 8 days demonstrated tumor growth inhibition in the GL26 xenograft tumor model [1].