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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
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).
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.
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.
Colletofragarone A2 V73177 Colletofragarone A2 181377-06-0 Colletofragarone A2 is extracted from the fungus Colletotrichum sp.
COTI-2 V3174 COTI-2 1039455-84-9 COTI-2 is an orally available, 3rd generation small molecule activator of the mutant p53 protein (a tumor suppressor).
FOXO4-DRI acetate V79511 FOXO4-DRI acetate FOXO4-DRI acetate is a cell-permeable (penetrable) peptide antagonist that blocks the interaction between FOXO4 and p53.
Ivaltinostat formic (CG-200745 formic) V76875 Ivaltinostat formic (CG-200745 formic) Ivaltinostat (CG-200745) formic is an orally bioactive pan-HDAC inhibitor (antagonist) with a hydroxamic acid moiety that binds zinc at the base of the catalytic pocket.
JNJ-26854165 (Serdemetan) V0013 JNJ-26854165 (Serdemetan) 881202-45-5 Serdemetan (formerly JNJ26854165; JNJ-26854165; JNJ 26854165), originally developed as an activator of p53, is now considered to be a novel, potent and orally bioactive antagonist of Human Double Minute-2 (HDM-2) ubiquitin ligase with antitumor activities.
Kevetrin HCl 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.
MDM2-IN-27 V88498 MDM2-IN-27 MDM2-IN-27 mainly targets MDM2 protein (Ki = 0.4 nM), activates the anti-tumor activity of p53 and induces cell apoptosis by blocking the negative regulation of MDM2 on p53.
MDM2-p53-IN-15 V80724 MDM2-p53-IN-15 MDM2-p53-IN-15 is an inhibitor (blocker/antagonist) of MDM2-p53 with IC50 of 26.1 nM.
MDM2/4-p53-IN-1 V78143 MDM2/4-p53-IN-1 MDM2/4-p53-IN-1 is a potent inhibitor of MDM2-p53 and MDM4-p53, with IC50s of 35.9 and 57.4 nM for MDM2-p53 and MDM4-p53, respectively.
MDM2/4-p53-IN-2 V88499 MDM2/4-p53-IN-2 MDM2/4-p53-IN-2 (2q) is a potent dual MDM2/ MDM4 inhibitor and p53 activator with IC50 values of 70.7 nM and 81.4 nM for MDM2-p53 and MDM4-p53 complexes, respectively.
MDM2/4-p53-IN-3 V88510 MDM2/4-p53-IN-3 MDM2/4-p53-IN-3 is a MDM2/4-p53 protein-protein interaction (PPI) inhibitor (IC50s: 18.5 nM, MDM2-p53; 14.8 nM, MDM4-p53).
MDMX/MDM2-IN-2 V80725 MDMX/MDM2-IN-2 MDMX/MDM2-IN-2 is a potent dual p53-MDM2/MDMX inhibitor (antagonist) with Ki of 0.23 μM and 2.45 μM for MDM2 and MDMX, respectively.
MI-773 (2'S,3R isomer, SAR-405838) V0021 MI-773 (2'S,3R isomer, SAR-405838) 1303607-60-4 MI-773 (2S,3R isomer, SAR405838) is a novel, potent, specific and orally bioavailable small molecule antagonist of MDM2/piro-oxindole HDM2 (Murine double minute 2/human double minute 2) with a Ki value of 0.88 nM.
MS78 V80841 MS78 MS78 is an acetylation-targeting chimera (AceTAC) that acetylates the p53 tumor suppressor protein.
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