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p53

p53

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.

p53 related products

Structure Cat No. Product Name CAS No. Product Description
(E/Z)-YLF-466D V121815 (E/Z)-YLF-466D 2097379-50-3 (E/Z)-YLF-466D is an AMPK activator.
1-吖丁啶硫代羧酸[1-(2-吡啶基)亚乙基]酰肼 V0017 NSC 319726 71555-25-4 NSC319726 is a novel and potent p53(R175) mutant reactivator with with potential anticancer activity.
2-苯乙炔磺酰胺 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.
4-异硫脲基丁腈盐酸盐 V4115 Kevetrin HCl 66592-89-0 Kevetrinhydrochloride (also known as thioureidobutyronitrile; 4-Isothioureidobutyronitrile hydrochloride; thioureidobutyronitrile hydrochloride; thioureido butyronitrile hydrochloride), is a water-soluble, small molecule activator of the tumor suppressor protein p53.
5-氯-2-(甲磺酰基)嘧啶-4-羧酸 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).
Altissimacoumarin F V128624 Altissimacoumarin F 1384897-64-6 Altissimacoumarin F is a terpenoid coumarin.
Anticancer agent 314 V128986 Anticancer agent 314 Anticancer agent 314 is a multi-target anticancer drug with microtubule polymerization inhibitory activity (IC50 = 6.35 μM) as well as human carbonic anhydrase IX (Ki = 27.1 nM) and XII (Ki = 20.9 nM) inhibitory activities.
Anticancer agent 68 V76056 Anticancer agent 68 2692652-36-9 Anticancer agent 68 is (Compound 12) is an anticancer agent.
Antitumor agent-150 V88501 Antitumor agent-150 Antitumor agent-150 (V10) is an anti-breast cancer agent and a PROTAC degrader of MDM2 (Red: Ganoderic acid A; Black: 4O-PEG linker; Blue: VHL ligand).
Antitumor agent-202 V129184 Antitumor agent-202 38470-63-2 Antitumor agent-202 is a stabilizer for the p53 Y220C mutant.
Apoptosis inducer 43 V129293 Apoptosis inducer 43 Apoptosis inducer 43 is an apoptosis inducer.
Apoptosis inducer 56 V129295 Apoptosis inducer 56 952306-31-9 Apoptosis inducer 56 is an apoptosis inducer.
Azurin p28 peptide TFA V88504 Azurin p28 peptide TFA Azurin p28 peptide TFA is a tumor-penetrating antitumor peptide.
BAY 1892005 V76057 BAY 1892005 2036352-13-1 BAY 1892005 is a modulator of p53 protein that acts on p53 aggregates and does not cause reactivation of mutant p53.
BRD6257 V130636 BRD6257 BRD6257 is an orally effective protein phosphatase inhibitor with Mg2+/Mn2+ dependent 1D PPM1D activity and an IC50 value of 5 nM.
CBL0137 HCl V3173 CBL0137 HCl 1197397-89-9 CBL0137 HCl, the hydrochloride salt of CBL-0137 (formerly Curaxin 137 or CBL 0137), is an inhibitor of the histone chaperone,FACT (facilitates chromatin transcription complex).
CDK2/MDM2-IN-1 V88505 CDK2/MDM2-IN-1 CDK2/MDM2-IN-1 (III-13) is a CDK2/MDM2 dual inhibitor with IC50 of 2.60 nM for CDK2.
Cenersen V131372 Cenersen 872847-66-0 Cenersen is an oligonucleotide that targets TP53.
Chlorphoxim V131560 Chlorphoxim 14816-20-7 Chlorphoxim is a broad-spectrum and highly effective insecticide.
CK2-TN03 V131849 CK2-TN03 313226-24-3 CK2-TN03 is an ATP-competitive casein kinase 2 (CK2) inhibitor with an IC50 of 165 nM and a Ki of 20 nM.
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