1. Apoptosis
  2. 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.

MDM-2/p53 相关产品 (45):

Cat. No. Product Name Effect Purity
  • HY-15676
    RG7388 Antagonist 99.97%
    RG7388 是一种有效的,具有选择性的 p53-MDM2 拮抗剂,IC50 值为 6 nM。
  • HY-15484
    Pifithrin-α hydrobromide Inhibitor 98.28%
    Pifithrin-α hydrobromide 是一种 p53 抑制剂,也用作芳香烃受体 (AhR) 激动剂。
  • HY-32735
    Triptolide Inhibitor 99.83%
    Triptolide 是一种热休克因子 (HSF1) 抑制剂,抑制 HSP90-CDC37 结合,且诱导 HSP90 乙酰化,也抑制 MDM2 表达,这种作用具有剂量依赖性,IC50 范围为 47 到 73 nM。
  • HY-10029
    Nutlin 3a Inhibitor 98.11%
    Nutlin (3a) 是一种鼠双微体 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 Inhibitor 99.73%
    AMG 232 是一种有效的 p53-MDM2 相互作用抑制剂,在 SJSA-1 细胞中,IC50 值为 9.1 nM。
  • HY-19896
    COTI-2 Activator 99.40%
    COTI-2 是可将突变型 p53 转化为野生型构象的小分子抗癌候选药物。
  • HY-18935A
    CBL0137 hydrochloride Activator 98.25%
    CBL0137 hydrochloride 是组蛋白分子伴侣 FACT 的抑制剂。CBL0137 hydrochlorideye 也可以激活 p53 并抑制 NF-κB,对于它们的 EC50 值分别为 0.37 和 0.47 μM。
  • HY-103640
    WR-1065 dihydrochloride Activator
    WR-1065 dihydrochloride 可以保护正常组织免受某些癌症药物的毒性作用,并通过 JNK 依赖性信号通路激活 p53
  • HY-15695
    Puromycin aminonucleoside Activator 98.31%
    Puromycin aminonucleoside 是一种氨基核苷类抗生素,为嘌呤霉素类似物,但并不影响蛋白质合成或诱导凋亡。
  • HY-10959
    RG7112 Inhibitor 99.94%
    RG7112 是临床上第一个 MDM2 抑制剂,Kd 值为 11 nM。
  • HY-15954
    NVP-CGM097 Inhibitor 98.32%
    NVP-CGM097 是一种有效的选择性 MDM2 抑制剂,作用于 hMDM2IC50 为 1.7±0.1 nM。
  • HY-50696
    Nutlin 3 Inhibitor 98.32%
    Nutlin 3 是一种有效的 p53-MDM2 抑制剂,Ki 为 90 nM。
  • HY-16702A
    Pifithrin-β hydrobromide Inhibitor 99.90%
    Pifithrin-β是有效地p53抑制剂,IC50值为23 μM。
  • HY-16664
    SJ-172550 Inhibitor >98.0%
    SJ-172550是MDMX的小分子抑制剂; 与野生型p53肽竞争性结合于MDMX的EC50值为5 μM。
  • HY-P0121
    ReACp53 Inhibitor 99.65%
    ReACp53是一个细胞渗透的肽,能够抑制p53 amyloid formation, 缓解在癌细胞中p53的功能。
  • HY-13424
    RITA Inhibitor
    RITA(NSC 652287)与nutlin-3相似,能干扰p53与Mdm2的相互作用,及诱导DNA-蛋白质和DNA-DNA交联。
  • HY-19980
    PRIMA-1Met Activator >98.0%
    PRIMA-1MET 是一种突变型 p53 复活剂,可恢复突变型 p53 的野生型构象和功能,并引发肿瘤细胞凋亡。PRIMA-1MET 还抑制硒蛋白硫氧还蛋白还原酶 1 (TrxR1)。
  • HY-15510B
    Tenovin 6 Hydrochloride Activator >98.0%
    Tenovin-6 Hydrochloride 是水溶的 SIRT1SIRT2 抑制剂,p53 的激活剂,同时能抑制 HDAC8 的活性,对 SirT1,SirT2,和 SirT3 的IC50 值分别为 21 μM,10 μM 和 67 μM。
  • HY-18986
    SAR405838 Inhibitor 98.95%
    SAR405838是一种高效的选择性MDM2抑制剂, 与MDM2结合, Ki值为0.88 nM。
  • HY-13423
    Tenovin-1 Activator 99.39%
    Tenovin-1 是 sirtuin 1sirtuin 2 的抑制剂,同时可激活 p53,在癌症研究中可能具有潜在的治疗作用。