| Bioactivity | MDMX/MDM2-IN-2 is a potent p53-MDM2/MDMX dual inhibitors with Kis of 0.23 μM and 2.45 μM for MDM2 and MDMX, respectively. MDMX/MDM2-IN-2 inhibits the binding of p53 and MDM2 proteins. MDMX/MDM2-IN-2 restores the function of p53 and enables cell cycle arrest and apoptosis. MDMX/MDM2-IN-2 inhibits cell migration and invasion. MDMX/MDM2-IN-2 has antitumor activity[1]. |
| Target | Ki: 0.23 μM (MDM2) and 2.45 μM (MDMX) |
| Invitro | MDMX/MDM2-IN-2 对 HCT116 和 SH-SY5Y 细胞表现出适度的抗增殖活性 (IC50 分别为 0.68 μM 和 0.54 μM)。MDMX/MDM2-IN-2 对正常人肺上皮 BEAS-2B 细胞和 LO2 肝细胞具有低细胞毒性 (IC50 分别为 17.96 μM 和 15.93 μM)[1]。 MDMX/MDM2-IN-2 (0.6-2.4 μM; 48 小时) 诱导 HCT116 和 SH-SY5Y 细胞凋亡[1]。 MDMX/MDM2-IN-2 (0.6-2.4 μM; 48 小时) 使细胞周期停滞在 G1 期[1]。 MDMX/MDM2-IN-2 (0.6-2.4 μM; 48 小时) 增加 p53 及其下游靶标 MDM2、MDMX、p21 和 cleaved-caspase3 的水平[1]。 MDMX/MDM2-IN-2 (0.4-0.8 μM) 显着抑制 HCT116 和 SH-SY5Y 细胞的集落形成、迁移和侵袭[1]。 Apoptosis Analysis[1] Cell Line: |
| Name | MDMX/MDM2-IN-2 |
| Formula | C28H25Cl3FN3O3 |
| Molar Mass | 576.87 |
| 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]. Hui-Juan Luo, et al. Structure-based discovery of novel α-aminoketone derivatives as dual p53-MDM2/MDMX inhibitors for the treatment of cancer. Eur J Med Chem. 2023 Apr 5;252:115282. |