1. Apoptosis
  2. MDM-2/p53

MDM-2/p53

The p53 tumor suppressor is a principal mediator of growth arrest, senescence, and apoptosis in response to a broad array of cellular damage. p53 is a short-lived protein that is maintained at low, often undetectable, levels in normal cells. Under stress conditions, the p53 protein accumulates in the cell, binds in its tetrameric form to p53-response elements and induces the transcription of various genes.

MDM-2 is transcriptionally activated by p53 and MDM-2, in turn, inhibits p53 activity in several ways. MDM-2 binds to the p53 transactivation domain and thereby inhibits p53-mediated transactivation. MDM-2 also contains a signal sequence that is similar to the nuclear export signal of various viral proteins and, after binding to p53, it induces its nuclear export. As p53 is a transcription factor, it needs to be in the nucleus to be able to access the DNA; its transport to the cytoplasm by MDM-2 prevents this. Finally, MDM-2 is a ubiquitin ligase, so is able to target p53 for degradation by the proteasome.

In many tumors p53 is inactivated by the overexpression of the negative regulators MDM2 and MDM4 or by the loss of activity of the MDM2 inhibitor ARF. The pathway can be reactivated in these tumors by small molecules that inhibit the interaction of MDM2 and/or MDM4 with p53. Such molecules are now in clinical trials.

View MDM-2/p53 Pathway Map

MDM-2/p53 相关产品 (47):

Cat. No. Product Name Effect Purity
  • HY-15484
    Pifithrin-α hydrobromide p53 Inhibitor 98.28%
    Pifithrin-α hydrobromide是 p53 抑制剂,可阻断其转录活性并阻止细胞凋亡。
  • HY-15676
    Idasanutlin MDM2 Inhibitor 99.97%
    RG7388 是一种有效,选择性的 MDM2 拮抗剂,能够抑制 p53-MDM2 的结合,IC50 值为 6 nM。
  • HY-10029
    Nutlin 3a MDM2 Inhibitor 98.11%
    Nutlin 3a 是 Nutlin-3 的活性异构体,为一种鼠双微体 2 (MDM2) 拮抗剂,抑制 MDM2-p53 相互作用,且稳定 p53 蛋白,因此诱导细胞周期停滞和细胞凋亡。
  • HY-12296
    AMG 232 MDM2 Inhibitor 99.73%
    AMG 232 是一种有效,选择性,可口服的 p53-MDM2 相互作用抑制剂,IC50 值为 0.6 nM,与 MDM2 结合的 Kd 为 0.045 nM。
  • HY-50696
    Nutlin 3 MDM2 Inhibitor 98.32%
    Nutlin 3 是一种有效的 p53-MDM2 抑制剂,Ki 为 90 nM。
  • HY-101266
    Milademetan MDM2 Inhibitor
    Mliademetan 是 MDM2 的特异性抑制剂,是可用于治疗急性髓性白血