| Bioactivity | MDM2-p53-IN-16 is a MDM2-p53 complex inhibitor with an IC50 value of 4.3 nM to dissociate human p53/MDM2 complex. MDM2-p53-IN-16 reactivates p53, and induces Glioblastoma Multiforme (GBM) cell apoptosis and cell-cycle arrest. MDM2-p53-IN-16 can be used for the cancer research[1]. | ||||||||||||
| Invitro | MDM2-p53-IN-16 (0.01 nM-100 μM；1 小时) 解离 MDM2-p53 相互作用，IC50 值为 4.3 nM[1]。MDM2-p53-IN-16 (1 µM；8 小时) 显著增加多形性成胶质细胞瘤细胞中 p53 的水平[1]。MDM2-p53-IN-16 (1 µM；6 小时) 增加 p53 靶基因 MDM2、PUMA 和 p21 在 U87MG 细胞中的 mRNA 水平[1]。MDM2-p53-IN-16 显示出结合移位蛋白 (TSPO) 的能力，Ki 值为 87.2 nM[1]。MDM2-p53-IN-16 (1 µM；24 小时) 诱导 U87MG 细胞早期和晚期凋亡，和细胞周期阻滞[1]。MDM2-p53-IN-16 (1-10000 nM；48 小时) 对 U87MG 和野生型 p53 U343MG 细胞具有抗增殖活性，IC50 值分别为 1.2 和 1.6 μM[1]。 Cell Proliferation Assay[1] Cell Line: | ||||||||||||
| Name | MDM2-p53-IN-16 | ||||||||||||
| CAS | 1917350-09-4 | ||||||||||||
| Formula | C32H33N3O5 | ||||||||||||
| Molar Mass | 539.62 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Daniele S, et al. Lead Optimization of 2-Phenylindolylglyoxylyldipeptide Murine Double Minute (MDM)2/Translocator Protein (TSPO) Dual Inhibitors for the Treatment of Gliomas. J Med Chem. 2016 May 26;59(10):4526-38. |
MDM2-p53-IN-16
CAS: 1917350-09-4 F: C32H33N3O5 W: 539.62
MDM2-p53-IN-16 is a MDM2-p53 complex inhibitor with an IC50 value of 4.3 nM to dissociate human p53/MDM2 complex. MDM2-p
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