| Description | 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 not only enhances HSP70 expression but also diminishes HER2 and phospho-Akt levels, and downregulates IFN-γ-induced PD-L1 expression in GL26 cells. Demonstrating efficacy against Temozolomide-sensitive and -resistant GBM cells, colon cancer, leukemia, non-small cell lung cancer, and other malignancies, MAO A/HSP90-IN-2 may also impede tumor immune evasion [1]. |
| In vitro | MAO A/HSP90-IN-2对包括小鼠和人类胶质瘤细胞、结肠癌、白血病和非小细胞肺癌细胞在内的多种肿瘤细胞线（GL26、U251S、U251R、U87MG、U373MG 和 LN229）具有显著的生长抑制效应，IC50值分别为0.49、1.09、0.26、0.36、0.89 和 0.31 μM[1]。在0.3至3 μM浓度范围内作用24小时后，MAO A/HSP90-IN-2（化合物4-C）能够提高GL26和U251R细胞中HSP70的表达水平，同时降低HER2和磷酸化AKT的表达[1]。此外，0.5至1 μM浓度作用24小时，该化合物能够抑制GL26细胞对IFN-γ刺激后PD-L1表达的增加[1]。 |
| In vivo | MAO A/HSP90-IN-2（化合物4-C）（25mg/kg，腹腔注射，连续8天）在GL26异种移植肿瘤模型中显示出明显的肿瘤生长抑制作用[1]。 |
| Target activity | MAO-A:4.58 μM, HSP90:0.016 μM |
| molecular weight | 458.98 |
| Molecular formula | C25H31ClN2O4 |
| CAS | 2927489-99-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |