An important mediator of growth arrest, senescence, and apoptosis in response to a wide range of cellular damage is the tumor suppressor protein p53. In healthy cells, the short-lived protein p53 is kept at very low levels that are frequently undetectable. When under stress, the p53 protein builds up in the cell, binds to p53-response elements in its tetrameric form, and triggers the transcription of a number of genes.
P53 causes MDM-2 to become transcriptionally active, and MDM-2 then inhibits p53 activity in a number of ways. MDM-2 inhibits p53-mediated transactivation by attaching to the p53 transactivation domain. After binding to p53, MDM-2 induces nuclear export because it has a signal sequence that is similar to the nuclear export signal of several viral proteins. Because p53 is a transcription factor, MDM-2's transport of it to the cytoplasm prevents it from accessing the DNA, which is necessary for its function. Finally, because MDM-2 is an ubiquitin ligase, it can direct the proteasome to target p53 for destruction.
The overexpression of the negative regulators MDM2 and MDM4 or the diminished activity of the MDM2 inhibitor ARF both inactivate p53 in many tumors. In these tumors, small molecules that block the interaction of MDM2 and/or MDM4 with p53 can cause the pathway to be reactivated. Trials on such molecules are currently being conducted.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
|
V0091 | Pifithrin-β (QB-102 and Cyclic-Pifithrin-α) | 60477-34-1 | Pifithrin-β (also known as QB102 and Cyclic-Pifithrin-α) is anovel and potentp53inhibitor with anIC50of 23 μM. |
|
V0092 | Pifithrin-β HBr (QB102; Cyclic Pifithrin-α) | 511296-88-1 | Pifithrin-βHBr (QB-102; Cyclic-Pifithrin-α), the hydrobromide salt ofPifithrin-β, is a potentp53inhibitor (IC50of 23 μM) andacell-permeable Cyclized analog of Pifithrin-α with higher stability and reduced cytotoxicity. |
|
V0020 | Pifithrin-μ (NSC-303580) | 64984-31-2 | Pifithrin-μ (NSC303580) is a novel and potent inhibitor of p53 binding and p53-mediated apoptosis with a Kd of 0.82 mM in vitro. |
|
V4118 | PK11000 | 38275-34-2 | PK11000 is a novel and potent p53-targeting compound andan alkylating agent with anti-tumor activities through activation of unstablep53 (tumor suppressor p53). |
|
V76565 | ReACp53 | ReACp53 can inhibit the formation of p53 amyloid and rescue the role of p53 in cancer/tumor cells. | |
|
V76055 | RETRA | 1036069-26-7 | RETRA is a mutant p53-dependent p73 activator that can inhibit cancer cells harboring mutant p53. |
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V0015 | RITA (NSC 652287) | 213261-59-7 | RITA (also known as NSC-652287) is a novel and potent inhibitor of p53-HDM-2 protein-protein interaction with potential anticancer activity. |
|
V76058 | S100A2-p53-IN-1 | 2766609-08-7 | S100A2-p53-IN-1 (compound 51) is an inhibitor (blocker/antagonist) of S100A2-p53 interaction. |
|
V12467 | SCH529074 | 922150-11-6 | SCH529074 is an orally bioactive p53 activator. |
|
V0016 | Tenovin-1 | 380315-80-0 | Tenovin-1, a small molecule compound discovered by a cell-based screen, is a novel and potent activator of p53 that protects against MDM2-mediated p53 degradation. |
|
V3038 | Tenovin-3 | 1011301-27-1 | Tenovin-3 is a small molecule activator of p53 transcriptional activity and an inhibitor of sirtuin. |
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V0022 | Tenovin-6 | 1011557-82-6 | Tenovin-6 is an analog of tenovin-1 with higher water-solubility and has potential anticancer activity. |
|
V3850 | Tenovin-6 HCl | 1011301-29-3 | Tenovin-6 is an analog of tenovin-1 with more water-soluble and it inhibits the protein deacetylase activities of SIRT1, SIRT2 and SIRT3 with IC50 value of 21 μM, 10 μM, and 67 μM, respectively. |
|
V81673 | UNP-6457 | UNP-6457 is a potent inhibitor of MDM2-p53 interaction with IC50 of 8.9 nM. |
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