| Hazard Information | Back Directory | [Uses]
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] sup >. | [in vivo]
MAO A/HSP90-IN-2(compound 4-C) (25 mg/kg for i.p., eight days) reduces tumor growth in GL26 orthotopic xenograft tumor models[1]. | Animal Model: | GL26 orthotopic xenograft tumor models[1] | | Dosage: | 25mg/kg | | Administration: | Intraperitoneal injection (i.p.) | | Result: | Reduced tumor growth inhibition (TGI%) by 59.8% compared to the control group. |
| [IC 50]
MAO-A: 4.58 μM (IC50); HSP90: 0.016 μM (IC50) | [References]
[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. DOI:10.1016/j.ejmech.2023.115459 |
|
|