Bioactivity | MAO A/HSP90-IN-2 (compound 4-C) is a dual inhibitor of HSP90and MAO A with the IC50 values of 0.016 and 4.58 μM, respectively. MAO A/HSP90-IN-2 increases HSP70 expression and reduces HER2 and phospho-Akt expression, and decreases IFN-γ induced PD-L1 expression in GL26 cells. MAO A/HSP90-IN-2 inhibits the growth of Temozolomide (HY-17364) -sensitive and -resistant GBM cells, colon cancer, leukemia, non-small cell lung and other cancers, and has potential to inhibit tumor immune escape[1]. |
Invitro | MAO A/HSP90-IN-2 抑制小鼠和人的胶质瘤细胞以及结肠癌、白血病和非小细胞肺癌细胞的生长 (GL26、U251S、U251R、U87MG、U373MG和LN229, IC50 值分别为 0.49、1.09、0.26、0.36、0.89 和 0.31 μM) [1]。MAO A/HSP90-IN-2(compound 4-C)(0.3~3 μM, 24h) 上调 GL26 和 U251R 细胞中 HSP70 的表达,下调 HER2、磷酸化 AKT 表达[1]。MAO A/HSP90-IN-2 (0.5 - 1 μM, 24 h) 抑制 GL26 细胞中 IFN-γ 诱导的 PD-L1 的上升[1]。 Western Blot Analysis [1] Cell Line: |
In Vivo | MAO A/HSP90-IN-2 (compound 4-C) (25mg/kg,腹腔注射,8天) 在 GL26 异种移植肿瘤模型中抑制肿瘤的生长[1]。 Animal Model: |
Name | MAO A/HSP90-IN-2 |
CAS | 2927489-99-2 |
Formula | C25H31ClN2O4 |
Molar Mass | 458.98 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. 1、Hui-Ju Tseng, et al. Design, synthesis, and biological activity of dual monoamine oxidase A and heat shock protein 90 inhibitors, N-Methylpropargylamine-conjugated 4-isopropylresorcinol for glioblastoma. European Journal of Medicinal Chemistry. Volume 256, 5 August 2023, 115459. [2]. Hui-Ju Tseng, et al. Design, synthesis, and biological activity of dual monoamine oxidase A and heat shock protein 90 inhibitors, N-Methylpropargylamine-conjugated 4-isopropylresorcinol for glioblastoma. European Journal of Medicinal Chemistry. Volume 256, 5 August 2023, 115459. |