1917350-09-4

1917350-09-4 structure
1917350-09-4 structure
  • Name: MDM2-p53-IN-16
  • Chemical Name: MDM2-p53-IN-16
  • CAS Number: 1917350-09-4
  • Molecular Formula: C32H33N3O5
  • Molecular Weight: 539.62
  • Catalog: Signaling Pathways Apoptosis MDM-2/p53
  • Create Date: 2023-04-17 20:32:53
  • Modify Date: 2024-01-14 19:47:10
  • 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].

Name MDM2-p53-IN-16
Description 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].
Related Catalog
In Vitro 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: U87MG, U343MG and T98G cell lines Concentration: 1-10000 nM Incubation Time: 48 hours Result: Inhibited cell proliferation of U87MG, U343MG and T98G cells. Apoptosis Analysis[1] Cell Line: U87MG cell line Concentration: 1 µM Incubation Time: 24 hours Result: Induced cell apoptosis of U87MG cells. Cell Cycle Analysis[1] Cell Line: U87MG, U343MG and T98G cell lines Concentration: 1-10000 nM Incubation Time: 48 hours Result: Induced cell cycle arrest progression in the G2/M-phase of U87MG cells.
References

[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.  

Molecular Formula C32H33N3O5
Molecular Weight 539.62