- Signaling Pathways
- Apoptosis
- 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.
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MDM-2/p53 Signaling Pathway
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Sulfabenzamide (Standard)
0 ImagesSulfabenzamide (N-Sulfanilylbenzamide) (Standard) is the analytical standard of Sulfabenzamide (HY-B0960). This product is intended for research and analytical applications. Sulfabenzamide is a sulfonamide antibacterial agent. Sulfabenzamide exhibit antibacterial activity against Staphylococcus aureus (ATCC 25923) and Escherichia coli (ATCC 8739). Sulfabenzamide can promote autophagic cell autophagy in breast cancer cells through p53/ DRAM pathway. Sulfabenzamide increases caspase-3 activity, deactivates PARP1 and DNA-PK, downregulates AKT1 and AKT2. Sulfabenzamide can be used for the researches of breast cancer and bacterial infections. -
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AQ-101
0 ImagesCat. No.: HY-119709CAS No.: 1353384-61-8AQ-101 is a MDM2 degrader. Upon binding to MDM2, it blocks the MDM2-MDM4 interaction, inducing autoubiquitination and proteasome-mediated degradation of MDM2. AQ-101 activates p53, upregulates downstream targets including p21 and PUMA, and induces apoptosis and cell cycle arrest in tumor cells. AQ-101 inhibits the progression of acute lymphoblastic leukemia in xenograft animal models. AQ-101 can be used for research related to acute lymphoblastic leukemia. -
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MIRA-1 (Standard)
0 ImagesCat. No.: HY-108639RCAS No.: 72835-26-8Synonyms: NSC 19630 (Standard)MIRA-1 (Standard) is the analytical standard of MIRA-1 (HY-108639). This product is intended for research and analytical applications. MIRA-1 is a maleimide analogue. MIRA-1 can induce apoptosis in mutant p53 cells via restoration of p53-dependent transcriptional transactivation. MIRA-1 has anticancer activity. -
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GO-Y078
0 ImagesCat. No.: HY-137059CAS No.: 1217503-60-0GO-Y078 is a curcumin (HY-N0005) analog. GO-Y078 activates p38/JNK1/2. GO-Y078 activates the MAPK pathway, Caspase 3/8/9, PARP, AP-1, DR5, and TP53, while inhibiting cIAP-1, XIAP, and NF-κB. GO-Y078 induces sub-G1/G2/M phase arrest and Apoptosis. GO-Y078 impairs angiogenesis. GO-Y078 can be used in research related to osteosarcoma, cervical cancer, oral squamous cell carcinoma, and peritoneal metastasis of gastric cancer. -
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HLI98C
0 ImagesCat. No.: HY-18327CAS No.: 317326-90-2HLI98C is a ubiquitin ligase inhibitor. HLI98C inhibits p53 ubiquitylation. HLI98C inhibits HDM2 auto-ubiquitylation. -
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Pretilachlor (Standard)
0 ImagesCat. No.: HY-B2035RCAS No.: 51218-49-6Pretilachlor (Standard) is the analytical standard of Pretilachlor (HY-B2035). This product is intended for research and analytical applications. Pretilachlor is a chloroacetamide herbicide with biological activities including endocrine disruption, oxidative stress induction, apoptosis induction, and immunotoxicity. Pretilachlor exerts its effects by interfering with hormone metabolism, inducing oxidative stress, activating apoptotic pathways, and inhibiting immune functions. Pretilachlor upregulates the transcription of P53, Mdm2, and Bbc3, and increases the activities of Caspase3 and Caspase9; it upregulates the transcription of genes in the HPG/HPT axis and the activity of aromatase; it induces oxidative stress, elevates ROS levels, and upregulates CAT, SOD, and GPX. Pretilachlor downregulates the transcription of CXCL-C1C, IL-1β, and IL-8. Pretilachlor disrupts the normal physiological processes and embryonic development of fish, exhibiting significant toxicity. Pretilachlor can be used in studies related to weeding, environmental pollution, and behavioral toxicity in fish. -
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N-Desmethyl clomipramine-d7
0 ImagesCat. No.: HY-12388SSynonyms: Desmethylclomipramine-d7; Norclomipramine-d7N-Desmethyl clomipramine-d7 (Desmethylclomipramine-d7; Norclomipramine-d7) is the deuterated-labeled N-Desmethyl clomipramine (HY-12388). N-Desmethyl clomipramine is the orally active major active metabolite of the tricyclic antidepressant Clomipramine (HY-B0457A), possessing multiple activities including anti-inflammatory, antioxidant, antibacterial, and antiparasitic effects. N-Desmethyl clomipramine blocks autophagosome-lysosome fusion, leading to the accumulation of LC3-II, p62, ATG7, WIPI2, and ATG5-12, reactivates the p53/p21 pathway, induces apoptosis through C-PARP and C-CAS3, and inhibits the proliferation, migration, and invasion of renal cancer cells. N-Desmethyl clomipramine inhibits LdTOPIA, inducing R-loop accumulation in the nucleus of Leishmania, ultimately causing parasite death. N-Desmethyl clomipramine can be used for research on depression, metastatic renal cell carcinoma, and leishmaniasis. -
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Pifithrin-α hydrobromide (Standard)
0 ImagesCat. No.: HY-15484RCAS No.: 63208-82-2Synonyms: Pifithrin hydrobromide (Standard); PFTα hydrobromide (Standard)Pifithrin-α (hydrobromide) (Standard) is the analytical standard of Pifithrin-α (hydrobromide). This product is intended for research and analytical applications. Pifithrin-α hydrobromide is a p53 inhibitor which blocks its transcriptional activity and prevents cells from apoptosis. Pifithrin-α hydrobromide is also an aryl hydrocarbon receptor (AhR) agonist. -
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dsP53-285 saRNA
0 ImagesCat. No.: HY-177375dsP53-285 saRNA is a small activating RNA (saRNA) that readily activates wild-type p53 expression by targeting its promoter. dsP53-285 saRNA suppresses bladder cancer cells growth and metastasis. -
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Pemrametostat (Standard)
0 ImagesSynonyms: GSK3326595 (Standard); EPZ015938 (Standard)GSK3326595 (Standard) is the analytical standard of GSK3326595 (HY-101563). This product is intended for research and analytical applications. GSK3326595 is a protein arginine methyltransferase 5 (PRMT5) inhibitor. GSK3326595 decreases SARS-CoV-2 infection, inhibits cancer cell proliferation and induces pro-inflammatory macrophage polarization and increases hepatic triglyceride levels without affecting atherosclerosis. GSK3326595 can be used for research of relapsed/refractory mantle cell lymphoma. -
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Alrizomadlin (Standard)
0 ImagesCat. No.: HY-101518RCAS No.: 1818393-16-6Synonyms: APG-115 (Standard); AA-115 (Standard)Alrizomadlin (Standard) is the analytical standard of Alrizomadlin (HY-101518). This product is intended for research and analytical applications. Alrizomadlin (APG-115) is an orally active MDM2 protein inhibitor binding to MDM2 protein with IC50 and Ki values of 3.8 nM and 1 nM, respectively. Alrizomadlin blocks the interaction of MDM2 and p53 and induces cell-cycle arrest and apoptosis in a p53-dependent manner. -
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SCH529074 (Standard)
0 ImagesCat. No.: HY-110088RCAS No.: 922150-11-6SCH529074 (Standard) is the analytical standard of SCH529074 (HY-110088). This product is intended for research and analytical applications. SCH529074 is a potent and orally active p53 activator. SCH529074 binds specifically and conformation-dependently to p53 DBD ( DNA binding domain) with a Ki of 1-2 μM in a saturable manner. SCH529074 restores mutant p53 function and interrupts HDM2-mediated ubiquitination of wild Type p53. SCH529074 can be used for the study of non-small-cell lung carcinoma (NSCLC). -
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RG7112 (Standard)
0 ImagesCat. No.: HY-10959RCAS No.: 939981-39-2Synonyms: RO5045337 (Standard) -
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Nutlin-3 (Standard)
0 ImagesNutlin-3 (Standard) is the analytical standard of Nutlin-3. This product is intended for research and analytical applications. Nutlin-3 is a commercial available p53-MDM2 inhibitor, with Ki of 90 nM. -
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PhiKan 083 (Standard)
0 ImagesCat. No.: HY-108637RCAS No.: 880813-36-5PhiKan 083 (Standard) is the analytical standard of PhiKan 083 (HY-108637). This product is intended for research and analytical applications. PhiKan 083 is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a Kd of 167 μM. PhiKan 083 can be used for cancer research. -
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Grosvenorine (Standard)
0 ImagesCat. No.: HY-N3031RCAS No.: 156980-60-8Grosvenorine (Standard) is the analytical standard of Grosvenorine. This product is intended for research and analytical applications. Grosvenorine is an orally active flavonoid glycoside found in S. grosvenorii. Grosvenorine exhibits antibacterial, antioxidant and antiinflammation activities. Grosvenorine can induce apoptosis and increases anti-apoptotic Bcl-2 protein expression and reduces pro-apoptotic P53 protein expression in gastric tissues. Grosvenorine enhances mucin/glycoprotein secretion, regulates gastric pH, and reduces gastric lesion incidence.Grosvenorine increases glutathione peroxidase, catalase, and SOD levels, reduces lipid peroxidation (MDA), and lowers TNF-α and IL-6 levels. Grosvenorine can be used for the researches of bacterial infection and Gastric ulcer. -
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RKS262
0 ImagesCat. No.: HY-113720CAS No.: 1041469-97-9RKS262 is an orally active cyclin/CDK inhibitor. RKS262 is also an apoptosis inducer and cell cycle regulator, exhibiting cytotoxic activity against cancer cells. RKS262 induces caspase-3 cleavage, ROS generation, SAPK/JNK activation, and upregulates the expression of p53, Bid, Bad, Bok, and p27. RKS262 inhibits the expression of Bcl-2, Mcl-1, Bcl-xL, p21, cyclin D1, cyclin B1, cdc-2, cyclin D4, and DNA-pk KU-80 subunit. RKS262 suppresses the phosphorylation of the IGF-1R/PI3K/PKC pathway, ras oncogene activity, and Cdk-6, while increasing total Akt expression. RKS262 induces G2/M or S phase cell cycle arrest, disrupts mitochondrial transmembrane potential, and reduces tumor burden in xenograft models. RKS262 is used in research on neuroblastoma and ovarian cancer. -
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Hexamethylene bisacetamide (Standard)
0 ImagesSynonyms: HMBA (Standard)Hexamethylene bisacetamide (Standard) is the analytical standard of Hexamethylene bisacetamide. This product is intended for research and analytical applications. Hexamethylene bisacetamide (HMBA) is a differentiation inducer and selective bromine domain inhibitor that can differentiate across the blood-brain barrier. Hexamethylene bisacetamide can induce tumor cell differentiation and inhibit cell proliferation, showing antitumor activity. Hexamethylene bisacetamide induces apoptosis by Notch1, Bcl-2 and p53 signaling pathways. In addition, Hexamethylene bisacetamide improves the obesity phenotype of mice. -
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YO-2
0 ImagesCat. No.: HY-183877CAS No.: 288254-44-4YO-2 is a plasmin inhibitor and TP53 upregulator with anti-tumor and apoptosis-inducing activities. YO-2 upregulates the expression of TP53 and the tumor-suppressive miR-103/107, downregulates LRP1, and induces cellular DNA fragmentation and caspase cascade activation. YO-2 effectively blocks the growth of melanoma. YO-2 has been widely used in studies related to melanoma and colon cancer. -
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Petunidin-3-O-glucoside chloride (Standard)
0 ImagesPetunidin-3-O-glucoside chloride (Standard) is the analytical standard of Petunidin-3-O-glucoside chloride (HY-N7832). This product is intended for research and analytical applications. Petunidin-3-O-glucoside chloride is a blood-brain barrier-penetrating tyrosinase inhibitor with an IC50 of 10.3 μM and a Ki of 9.0 μM. Petunidin-3-O-glucoside also acts as an α-glucosidase inhibitor with an IC50 of 218.2 µM. Petunidin-3-O-glucoside chloride inhibits the SIRT3/p53-mediated mitochondrial pathway and the PI3K/Akt-ERK pathway, suppresses glycolysis, and induces cell apoptosis. Petunidin-3-O-glucoside chloride scavenges ROS to exert antioxidant activity. It can be used in research related to glioblastoma multiforme, skin anti-aging and whitening, as well as obesity. -
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p53 is at the centre of biological interactions that translates stress signals into cell cycle arrest or apoptosis. Upstream signaling to p53 increases its level and activates its function as a transcription factor in response to a wide variety of stresses, whereas downstream components execute the appropriate cellular response.
Cell Stress: p53 induction by acute DNA damage begins when DNA double-strand breaks trigger activation of ATM, a kinase that phosphorylates the CHK2 kinase, or when stalled or collapsed DNA replication forks recruit ATR, which phosphorylates CHK1. p53 is a substrate for both the ATM and ATR kinases, as well as for CHK1 and CHK2, which coordinately phosphorylate p53 to promote its stabilization. These phosphorylation events are important for p53 stabilization, as some of the modifications disrupt the interaction between p53 and its negative regulators MDM2 and MDM4. MDM2 and MDM4 bind to the transcriptional activation domains of p53, thereby inhibiting p53 transactivation function, and MDM2 has additional activity as an E3 ubiquitin ligase that causes proteasome-mediated degradation of p53. Phosphorylation also allows the interaction of p53 with transcriptional cofactors, which is ultimately important for activation of target genes and for responses such as cell cycle arrest, DNA repair, apoptosis and senescence. Non-receptor tyrosine kinase c-Abl can also be activated by DNA damage. Then the JNK/p38 is activated and leads to p53 activation[1][2].
Oncogenic signaling: The response to oncogene activation depends on the binding of ARF to MDM2. ARF is normally expressed at low levels in cells. Inappropriately increased E2F or Myc signals, stemming from oncogene activation, leads to the increased expression of ARF, which inhibits MDM2 by blocking its E3 ubiquitin ligase activity, uncoupling the p53-MDM2 interaction, thereby segregating it from nucleoplasmic p53[3].
The PI3K-Akt pathway activates MDM2 and increases the ubiquitination of p53.
Reference:
[1]. Chène P, et al. Inhibiting the p53-MDM2 interaction: an important target for cancer therapy. Nat Rev Cancer. 2003 Feb;3(2):102-9.
[2]. Brown CJ, et al. Awakening guardian angels: drugging the p53 pathway. Nat Rev Cancer. 2009 Dec;9(12):862-73.
[3]. Polager S, et al. p53 and E2f: partners in life and death. Nat Rev Cancer. 2009 Oct;9(10):738-48. doi: 10.1038/nrc2718.