p53

Sigaling Pathway Map

Research Area

Inhibitory Selectivity

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Notes:
2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Catalog No. Information Product Use Citations Product Validations
S2929

Pifithrin-α (PFTα)

Pifithrin-α is an inhibitor of p53, inhibiting p53-dependent transactivation of p53-responsive genes.

S8187New

ReACp53

ReACp53 is a cell-penetrating peptide, designed to inhibit p53 amyloid formation, resues p53 function in cancer cell lines and in organoids derived from high-grade serous ovarian carcinomas (HGSOC).

S8149New

NSC348884

NSC348884, as a nucleophosmin inhibitor, inhibit cell proliferation and induce apoptosis in various cancer cell lines with IC50 values ranging from 1.4-4 µM.

S2930

Pifithrin-μ

Pifithrin-μ is a specific p53 inhibitor by reducing its affinity to Bcl-xL and Bcl-2, and also inhibits HSP70 function and autophagy.

S1172

JNJ-26854165 (Serdemetan)

JNJ-26854165 (Serdemetan) acts as a HDM2 ubiquitin ligase antagonist and also induces early apoptosis in p53 wild-type cells, inhibits cellular proliferation followed by delayed apoptosis in the absence of functional p53. Phase 1.

S2678

NSC 207895

NSC 207895 suppresses MDMX with IC50 of 2.5 μM, leading to enhanced p53 stabilization/activation and DNA damage, and also regulates MDM2, an E3 ligase.

S2781

RITA (NSC 652287)

RITA (NSC 652287) induces both DNA-protein and DNA-DNA cross-links with no detectable DNA single-strand breaks, and also inhibits MDM2-p53 interaction by targeting p53.

S8000

Tenovin-1

Tenovin-1 protects against MDM2-mediated p53 degradation, which involves ubiquitination, and acts through inhibition of protein-deacetylating activities of SirT1 and SirT2.

S7724New

APR-246 (PRIMA-1MET)

APR-246, also known as PRIMA-1MET, is a small organic molecule that has been shown to restore tumour-suppressor function primarily to mutant p53 and also to induce cell death in various cancer types.

S7723New

PRIMA-1

PRIMA-1 is a mutant p53 reactivator. It induces apoptosis and inhibits growth of human tumors with mutant p53.

S8106New

NSC59984

NSC59984 is a p53 pathway activator via induction of mutant p53 protein degradation and p73 activation.

S7149

NSC 319726

NSC319726 is a p53(R175) mutant reactivator, exhibits growth inhibition in cells expressing mutant p53, with IC50 of 8 nM for p53(R175) mutant, shows no inhibition for p53 wild-type cells.

S7649

MI-773 (SAR405838)

MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.

S4900

Tenovin-6

Tenovin-6 is a small molecule activator of p53 transcriptional activity.

Catalog No. Information Product Use Citations Product Validations
S2929

Pifithrin-α (PFTα)

Pifithrin-α is an inhibitor of p53, inhibiting p53-dependent transactivation of p53-responsive genes.

S8187New

ReACp53

ReACp53 is a cell-penetrating peptide, designed to inhibit p53 amyloid formation, resues p53 function in cancer cell lines and in organoids derived from high-grade serous ovarian carcinomas (HGSOC).

S8149New

NSC348884

NSC348884, as a nucleophosmin inhibitor, inhibit cell proliferation and induce apoptosis in various cancer cell lines with IC50 values ranging from 1.4-4 µM.

S2930

Pifithrin-μ

Pifithrin-μ is a specific p53 inhibitor by reducing its affinity to Bcl-xL and Bcl-2, and also inhibits HSP70 function and autophagy.

Catalog No. Information Product Use Citations Product Validations
S1172

JNJ-26854165 (Serdemetan)

JNJ-26854165 (Serdemetan) acts as a HDM2 ubiquitin ligase antagonist and also induces early apoptosis in p53 wild-type cells, inhibits cellular proliferation followed by delayed apoptosis in the absence of functional p53. Phase 1.

2014, 4:4664

2015, 23(5):857-65

2014, 10.1002/hed.23822

S2678

NSC 207895

NSC 207895 suppresses MDMX with IC50 of 2.5 μM, leading to enhanced p53 stabilization/activation and DNA damage, and also regulates MDM2, an E3 ligase.

S2781

RITA (NSC 652287)

RITA (NSC 652287) induces both DNA-protein and DNA-DNA cross-links with no detectable DNA single-strand breaks, and also inhibits MDM2-p53 interaction by targeting p53.

2015, 10.1038/nchembio.1986

2014, 10.1038/onc.2014.37

S8000

Tenovin-1

Tenovin-1 protects against MDM2-mediated p53 degradation, which involves ubiquitination, and acts through inhibition of protein-deacetylating activities of SirT1 and SirT2.

S7724New

APR-246 (PRIMA-1MET)

APR-246, also known as PRIMA-1MET, is a small organic molecule that has been shown to restore tumour-suppressor function primarily to mutant p53 and also to induce cell death in various cancer types.

S7723New

PRIMA-1

PRIMA-1 is a mutant p53 reactivator. It induces apoptosis and inhibits growth of human tumors with mutant p53.

S8106New

NSC59984

NSC59984 is a p53 pathway activator via induction of mutant p53 protein degradation and p73 activation.

S7149

NSC 319726

NSC319726 is a p53(R175) mutant reactivator, exhibits growth inhibition in cells expressing mutant p53, with IC50 of 8 nM for p53(R175) mutant, shows no inhibition for p53 wild-type cells.

S7649

MI-773 (SAR405838)

MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.

S4900

Tenovin-6

Tenovin-6 is a small molecule activator of p53 transcriptional activity.

2015, 10.1038/nbt.3130

Tags: p53 apoptosis | p53 inhibition | p53 cancer | p53 mutation | p53 protein | p53 pathway | p53 activation | p53 phosphorylation | p53 activity | p53-dependent apoptosis | p53 apoptosis pathway | p53 cancer therapy | p53-independent apoptosis | p53-mdm2 interaction | p53-p21 pathway | p53-mdm2 pathway | p53 protein structure | p53 protein function | p53 cleavage | p53 inhibitor review