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
V76056 Anticancer agent 68 2692652-36-9
V76057 BAY 1892005 2036352-13-1
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).
V73177 Colletofragarone A2 181377-06-0
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).
V79511 FOXO4-DRI acetate
V76875 Ivaltinostat formic (CG-200745 formic)
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.
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.
V80724 MDM2-p53-IN-15
V78143 MDM2/4-p53-IN-1
V80725 MDMX/MDM2-IN-2
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.
V80841 MS78
V26035 MS7972 352553-42-5 MS7972 is a novel and potent CREBBP inhibitor.
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.
V0017 NSC 319726 71555-25-4 NSC319726 is a novel and potent p53(R175) mutant reactivator with with potential anticancer activity.
V0018 NSC59984 803647-40-7 NSC59984 is a novel and potent activator of p53 with potential anticancer activity.
V81028 p53 (17-26), FITC labeled
V0014 Pifithrin-α (PFTα) HBr 63208-82-2 Pifithrin-α HBr ((PFTα hydrobromide; PFT-α) is a novel and potent inhibitor of p53, acting by inhibiting p53 protein transcription and p53-dependent transactivation of p53-responsive genes.
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