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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
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.
MI773 (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.
MS7972 V26035 MS7972 352553-42-5 MS7972 is a small molecule that blocks the binding of human p53 to CREB.
N-[[[4-(乙酰氨基)苯基]氨基]硫代甲酰]-4-叔丁基苯甲酰胺 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.
NSC 146109 HCl V5034 NSC 146109 HCl 59474-01-0 NSC 146109 (NSC-146109) HCl, the hydrochloride salt ofNSC-146109, is a novel and potent small-molecule p53 activator that targets MDMX, it has the potential in treating breast cancer.
NSC-59984 V0018 NSC59984 803647-40-7 NSC59984 is a novel and potent activator of p53 with potential anticancer activity.
NSC90616 V88508 NSC90616 NSC90616 is a p53 mutation rescue compound.
p53 (17-26), FITC labeled V81028 p53 (17-26), FITC labeled p53 (17-26), FITC labeled is a biologically active peptide.
p53 Activator 12 V88502 p53 Activator 12 2746374-04-7 p53 Activator 12 (compound 510B) is a potent p53 activator.
p53 Activator 13 V104410 p53 Activator 13 p53 Activator 13 (Compound 11) is a 6mA methyltransferase CamA inhibitor and p53 activator.
p53-MDM2-IN-2 V88509 p53-MDM2-IN-2 1542066-69-2 p53-MDM2-IN-2 (Compound 5q) is an orally active p53-MDM2 inhibitor with a Ki value of 0.25 μM.
p53-MDM2-IN-3 V88517 p53-MDM2-IN-3 1542066-74-9 p53-MDM2-IN-3 (Compound 5s) is an orally active p53-MDM2 inhibitor with a Ki value of 0.25 μM.
PAWI-2 V88511 PAWI-2 1448427-02-8 PAWI-2 is a p53 activator and Wnt inhibitor.
Phage-derived 12/1 peptide V88503 Phage-derived 12/1 peptide 186180-20-1 Phage-derived 12/1 peptide exerts antitumor activity by targeting MDM2 and MDMX, thereby disrupting MDM2-p53 and MDMX-p53 interactions with IC50 of 0.15 and 1.25 μM.
PNC-27 acetate V88518 PNC-27 acetate PNC-27 acetate is a chimeric p53-penetrating peptide that binds to HDM-2 in a p53 peptide-like structure, inducing selective membrane pore formation and leading to cancer cell lysis.
PROTAC LZK-IN-1 V105166 PROTAC LZK-IN-1 2763268-64-8 PROTAC LZK-IN-1 (compound 21A) is a PROTAC that targets and degrades LZK (leucine zipper kinase, encoded by MAP3K13).
ReACp53 V76565 ReACp53 ReACp53 can inhibit the formation of p53 amyloid and rescue the role of p53 in cancer/tumor cells.
RETRA 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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