p53

p53 (TP53) is a transcription factor whose protein levels and post-translational modification state alter in response to cellular stress (e.g. hypoxia, DNA and spindle damage). Activation of p53 occurs by several mechanisms including phosphorylation by ATM, ATR, Chk1 and MAPKs.

Products
Background
Literature
Pathways
Gene Data

Inhibitors

Cat No Product Name / Activity
1267 Pifithrin-α hydrobromide
p53 inhibitor. Also aryl hydrocarbon receptor agonist
3843 Cyclic Pifithrin-α hydrobromide
p53 inhibitor
2653 Pifithrin-μ
Inhibitor of p53-mitochondrial binding

Activators

Cat No Product Name / Activity
3503 HLI 373
Hdm2 inhibitor; activates p53-dependent transcription
2185 NSC 146109 hydrochloride
Cell-permeable, genotype-selective antitumor agent; activates p53-dependent transcription
5065 NSC 319726
Reactivator of mutant p53
2936 NSC 66811
MDM2 inhibitor. Disrupts MDM2-p53 interaction
3984 Nutlin-3
MDM2 antagonist; inhibits MDM2-p53 interaction
6075 Nutlin 3a
MDM2 antagonist; active enantiomer of Nutlin-3 (Cat. No. 3984)
2443 RITA
p53-MDM2 interaction inhibitor; antitumor
3929 SJ 172550
MDMX inhibitor. Disrupts MDMX-p53 interaction
5332 SP 141
High affinity MDM2 inhibitor
3365 Tenovin-1
Activates p53 transcriptional activity
3356 WR 1065
p53 activator. Also ROS scavenger

Other

Cat No Product Name / Activity
5417 BMH 21
p53 pathway activator; also RNA polymerase 1 inhibitor
3023 CP 31398 dihydrochloride
p53-stabilizing agent
3362 MIRA-1
Restores mutant p53 activity; proapoptotic
4326 PhiKan 083
p53 stabilizing agent
4396 Piperlongumine
Induces apoptosis; increases p53 and ROS levels in cancer cells
4761 Plumbagin
Induces p53 Ser10 phosphorylation; anticancer
1862 PRIMA-1
Restores mutant p53 activity; induces apoptosis
3710 PRIMA-1MET
Restores mutant p53 activity
3214 RETRA hydrochloride
Antitumor agent; suppresses mutant p53-bearing cancer cells
4240 SCH 529074
Restores mutant p53 activity

p53 (aka TP53) is a transcription factor whose protein levels and post-translational modification state alter in response to cellular stress (such as DNA damage, hypoxia and spindle damage). Activation of p53 begins through a number of mechanisms including phosphorylation by ATM, ATR, Chk1 and MAPKs. MDM2 is a ubiquitin ligase that binds p53 and targets p53 for proteasomal degradation.

Phosphorylation, p14ARF and USP7 prevent MDM2-p53 interactions, leading to an increase in stable p53 tetramers in the cytoplasm. Further modifications such as methylation and acetylation lead to an increase in p53 binding to gene specific response elements. p53 regulates a large number of genes (>100 genes) that control a number of key tumor suppressing functions such as cell cycle arrest, DNA repair, senescence and apoptosis. Whilst the activation of p53 often leads to apoptosis, p53 inactivation facilitates tumor progression; inactivating p53 mutations occur in over 50% of cancers.

Literature for p53

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Cell Cycle & DNA Damage Repair

Cell Cycle & DNA Damage Repair Poster

In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.

Pathways for p53

p53

p53 Signaling Pathway

p53 signaling plays an important role in the co-ordination of the cellular response different types of stress such as DNA damage and hypoxia. The downstream signals lead to apoptosis, senescence and cell cycle arrest.

p53 Gene Data

Species Gene Symbol Gene Accession No. Protein Accession No.
Human TP53 NM_000546 P04637
Mouse Trp53 NM_011640 P02340
Rat Tp53 NM_030989 P10361