p53

p53-Mdm2 inhibitor 4 inhibits the p53-MDM2 protein-protein interaction.

p53 Activator 7 is a highly potent and cell-permeable activator of the p53 mutation Y220C (MDM-2/p53), which induces apoptosis.

This peptide is amino acids 17 to 26 fragment of p53, the Mdm-2 binding domain of p53 known also as p53N. This sequence contains all of the residues that contact the binding domain of Mdm-2.

p53 tumor suppressor fragment (232-240) is a peptide with the sequence H2N-Lys-Tyr-Met-Cys-Asn-Ser-Ser-Cys-Met-OH, MW= 1066.3. p53 is a tumor suppressor protein that in humans is encoded by the TP53 gene. p53 is crucial in multicellular organisms, where i

Tetrofosmin is a phosphine developed to overcome the non-target uptake of radioligands by the generation of hetero-atomic compounds.

p53 and MDM2 proteins-interaction-inhibitor (racemic) is an inhibitor of the interaction between p53 and MDM2 proteins.

Tumor protein p53 binding protein (53BP1) has been identified in a yeast two-hybrid screen as a protein that interacts with the central DNA–binding domain of p532. Similar to breast cancer susceptibility gene 13, 4 (BRCA1; 53BP1 enhances p53-dependent tra

Mutant p53 modulator-1 is a mutant p53 modulator. mutant p53 modulator-1 is able to hinder the progression of cancers containing p53 mutations.

p53-MDM2-IN-1 (Example 30), an inhibitor targeting the p53-MDM2 X protein interaction, exhibits a K i value of 23.35 µM. This compound holds potential for applications in anti-tumor research.

p53 Activator 2 (compound 10ah) intercalates into DNA, causing significant DNA double-strand breaks and upregulates the expression of p53, p-p53, CDK4, and p21, leading to cell cycle arrest at the G2/M phase. It induces apoptosis, significantly reduces the expression of anti-apoptosis proteins Bcl-2, Bcl-xL, and cyclin B1 levels, and exhibits anti-proliferative activity against MGC-803 cells with an IC50 of 1.73 μM. Furthermore, p53 Activator 2 demonstrates potent anticancer effectiveness in MGC-803 xenograft tumor models [1].

MDM2-p53-IN-1b is the MDM2-p53 interaction inhibitor.

rel-MDM2/4-p53-IN-3 is an MDM2/4-p53 protein-protein interaction (PPI) inhibitor that acts on MDM2-p53 and MDM4-p53 with IC50 values of 18.5 nM and 14.8 nM, respectively. rel-MDM2/4-p53-IN-3 can be used to study cancers, such as colon cancer.

p53 Activator 3 is a potent activator of p53, demonstrating notable efficacy with an SC150 value of less than 0.05 mM. It effectively binds to mutant p53, reinstating its DNA-binding capability, and exhibits anti-tumor activity.

P53 Activator 5 is a potent activator of p53, exhibiting a SC150 value of less than 0.05 mM. It effectively binds to mutant p53, restoring its DNA-binding capability. Additionally, P53 Activator 5 demonstrates significant anti-tumor activity.

p53 and MDM2 proteins-interaction-inhibitor dihydrochloride is a interaction inhibitor between p53 and MDM2 proteins.

S100A2-p53-IN-1 (compound 51), an inhibitor of S100A2-p53 interactions, targets S100A2, a Ca 2+ binding protein involved in cell signaling and commonly upregulated in pancreatic cancer. This compound effectively inhibits the growth of the MiaPaCa-2 pancreatic cancer cell line, showing a growth inhibition (GI 50) range of 1.2-3.4 μM [1].

MDM2/4-p53-IN-2 (2q) is a potent dual inhibitor of MDM2/MDM4 and activator of p53, demonstrating IC50 values of 70.7 nM for MDM2-p53 and 81.4 nM for MDM4-p53 complexes. It facilitates cell cycle regulation, promotes apoptosis, and exhibits anticancer properties [1].

MDM2/4-p53-IN-3, an inhibitor of MDM2/4-p53 protein-protein interactions (PPIs), exhibits potent activity with IC50 values of 18.5 nM for MDM2-p53 and 14.8 nM for MDM4-p53. This compound is applicable in cancer research, including studies on colon cancer [1].

p53 CBS (p53 Consensus binding sequence), a biologically active peptide, functions as the p53 consensus DNA binding site.

MDM2-p53-IN-16 is a potent inhibitor of the MDM2-p53 complex, exhibiting an IC 50 value of 4.3 nM for the dissociation of the human p53/MDM2 complex. It effectively reactivates p53, leading to apoptosis and cell-cycle arrest in Glioblastoma Multiforme (GBM) cells, positioning it as a valuable agent for cancer research.

p53-HDM2-IN-1 is a potent inhibitor of the p53-HDM2 protein-protein interaction, demonstrating an inhibitory concentration (IC 50) of 0.103 μM. This compound has significant applications in cancer research.

rel-MDM2/4-p53-IN-2 (2q) is a potent dual MDM2/MDM4 inhibitor and p53 activator that acts on both the MDM2-p53 complex (IC50: 70.7 nM) and the MDM4-p53 complex (IC50: 81.4 nM). rel-MDM2/4-p53-IN-2 is capable of regulating cell cycle, induce apoptosis, and exhibit anti-cancer effects.

ReACp53 acetate could inhibit p53 amyloid formation and rescue p53 function in cancer cell lines.

STIMA-1 (2-Vinylquinazolin-4-ol), an active compound, can restore the activity of p63. STIMA-1 can stimulate the proliferation and differentiation of keratinocytes.

MIRA-1 (WRN Helicase Inhibitor) is a restorer of wild-type p53 conformation/cellular function and selectively inhibits Werner syndrome WRN helicase activity with an IC50 of 20 µM.

Alrizomadlin (APG-115) is an orally active inhibitor of MDM2 with IC50 of 3.8 nM and Ki of 1 nM, respectively[1]. Alrizomadlin blocks the interaction of MDM2 and p53 and induces cell-cycle arrest and apoptosis in a p53-dependent manner.

Navtemadlin (AMG232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction (IC50: 0.6 nM). It binds to MDM2 with a Kd of 0.045 nM.

CBL0137 hydrochloride (Curaxin-137 hydrochloride) activates p53 and inhibits NF-kB (EC50: 0.37/0.47 μM) in the cell-based p53 and NF-kB reporter assays, respectively. It also suppresses histone chaperone FACT.

1. Chelidonine (Stylophorin) isolated from Chelidonium majus efficiently induced apoptosis in HeLa cells through possible alteration of p38-p53 and AKT/PI3 kinase signalling pathways. 2. Chelidonine is a promising model compound for overcoming MDR and for enhancing cytotoxicity of chemotherapeutics, especially against leukaemia cells, its efficacy needs to be confirmed in animal models. 3. Chelidonine may be a potential therapeutic agent against metastasis of invasive human cancer cells, exhibits antimigratory and antiinvasive effects in MDA-MB-231 cells, by suppressing COL-induced integrin signaling, through inhibiting the formation of the IPP complex and subsequent downregulation of IPP downstream signaling molecules, such as Akt and ERK1/2.

Etoposide (VP-16-213) is a topoisomerase II inhibitor that inhibits DNA synthesis by forming a complex with topoisomerase II and DNA (IC50=60.3 μM). Etoposide has antitumor activity and induces apoptosis and autophagy.

Flubendazole (Flumoxane) is available OTC in Europe that is an anthelmintic using to treat worm infection in humans.

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).

Penicillamine (Artamine), possessing antineoplastic properties, induces apoptosis by a p53-mediated mechanism and inhibits angiogenesis by chelating with copper, a cofactor for angiogenesis. Artamine is a beta dimethyl analog of the amino acid cysteine. As a degradation product of penicillin antibiotics, Artamine chelates with heavy metals and increases their urinary excretion.

Sarmustine (SarCNU) is an alkylating agent with anticancer activity that inhibits the growth of prostate cancer cells via p53-dependent and p53-independent pathways.Sarmustine mediates the selection of P140K methylguanine-DNA-methyltransferase-transduced human CD34(+) cells in vitro.

PUMA BH3 acetate (PUMA BH3 Free base) is a p53 positive regulator of apoptosis (PUMA) BH3 domain polypeptide that acts as a direct activator of Bak with a Kd of 26 nM.

AK301 is a potent and selective inhibitor of tubulin polymerization and an effective sensitizer of cancer cells to apoptotic ligands (EC50 < 200 nM). Colon cancer cells arrested in mitosis with AK301 readily underwent a p53-dependent apoptosis following compound withdrawal and arrest release.

CT-1 is a DNA minor groove ligand and causes p53-dependent breast cancer cell apoptosis.

SF5 is an inhibitor of the apoptosis pathway. Which is through the JNK-p53-caspase apoptotic cascade.

RAPTA-C induces EAC cell cycle arrest and apoptosis via the mitochondrial and p53-JNK pathways, and can be used in the study of breast and ovarian cancer.

Proteasome inhibitor IX (PS-IX) is an inhibitor of chymotrypsin-like activity of the 20S proteasome (IC50 ~1 μM). Proteasome inhibitor IX shows potent anticancer activity. Proteasome inhibitor IX exhibits HCT116 p53+/+ cells growth inhibitory activity(IC50 = 1.49 μM).

MB710, an aminobenzothiazole derivative, stabilizes the oncogenic p53 mutation Y220C by binding tightly to the Y220C pocket, enhancing the stability of p53-Y220C with a dissociation constant (Kd) of 4.1 μM. This compound exhibits anticancer activity in cell lines harboring the p53-Y220C mutation [1].

RO-5963 is a dual inhibitor of p53-MDM2 and p53-MDMX (IC50s: ~17 nM and ~24 nM, respectively).

DPBQ (ZINC1620467) is a p53 activator. DPBQ could activate p53 and trigger apoptosis in a polyploid-specific manner, without inhibition of topoisomerase or bind DNA.

Pentamidine dimesylate is an inhibitor of calcium-dependent complex formation with p53 [(Ca)S100B-p53) in malignant melanoma (MM). Pentamidine dimesylate restores p53 tumor suppressor activity in vivo.

JGB1741 (ILS-JGB-1741) is a potent and selective inhibitor of SIRT1 with an IC50 of 15 μM. JGB1741 modulates Bax/Bcl2 ratio, cytochrome c release and PARP cleavage and increases the acetylated p53 levels leading to p53-mediated apoptosis. JGB1741 can be used in studies about breast cancer.

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

NSC-697923 (2-[(4-methylphenyl)sulfonyl]-5-nitrofuran), a potent inhibitor of UBE2N (ubiquitin-conjugating enzyme E2 N, Ubc13), exhibits its role in inducing cell death in neuroblastoma (NB) cells through two distinct mechanisms. In p53 wild-type NB cells, NSC-697923 promotes the nuclear importation of p53, thereby triggering cell death. Meanwhile, in p53 mutant NB cells, NSC-697923 activates the JNK-mediated apoptotic pathway, leading to cell death. Additionally, NSC-697923 inhibits DNA damage and NF-κB signaling, further contributing to its antitumor activity.

Droloxifene (3-Hydroxytamoxifen), a tamoxifen derivative, is an oral active and selective estrogen receptor modulator.Droloxifene induced p53 expression and apoptosis in McF-7 cells.Fluroxifene has anti-estrogen and anti-implantation effects.Fluroxifene prevented bone loss in ovariectomized rats.

Roslin 2 bromide (Benzylhexamethylenetetramine bromide) is a p53 reactivator that disrupts the binding of FAK and p5. Roslin 2 bromide exhibits anticancer effects.

Vesnarinone (Arkin) (INN) is a mixed phosphodiesterase 3 inhibitor and ion-channel modifier that has modest, dose-dependent, positive inotropic activity, but minimal negative chronotropic activity. It also suppresses cell proliferation and induces apoptosis by inducing the expression of p21, an inhibitor of cyclin-dependent kinase activity in p53-mediated cell cycle arrest.