p53

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  1. PhiKan 083 hydrochloride is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a Kd of 167 μM, and a relative binding affinity (Kd) of 150 μM in Ln229 cells.
  2. p53 Activator

    C16-Ceramide is a natural small molecule that acts as a p53 activator by directly and selectively binding to the protein. This compound is known to induce apoptosis in various cancer cell lines, making it a valuable tool for research in cancer biology and therapeutic development. Its ability to modulate p53 activity facilitates investigations into cellular stress responses and the mechanisms underlying tumor suppression.
  3. p53 Inhibitor

    p-nitro-Pifithrin-α is a potent inhibitor of the p53 tumor suppressor protein. This cell-permeable compound effectively suppresses p53-mediated TGF-β1 expression in HK-2 kidney cells and prevents the activation of caspase-3 induced by Zika virus strains. Additionally, p-nitro-Pifithrin-α demonstrates protective effects against steatosis and liver injury in high-fat diet models, positioning it as a valuable tool in the study of non-alcoholic fatty liver disease and p53-related pathways.
  4. p53 Activator/Wnt Inhibitor

    PAWI-2 is a p53 activator and Wnt inhibitor that targets β3-KRAS signaling independently of KRAS. This compound selectively inhibits the phosphorylation of TBK1, resulting in the activation of apoptotic pathways, evidenced by increased caspase-3/7 activity and PARP cleavage. Additionally, PAWI-2 facilitates the translocation of optineurin into the nucleus and induces G2/M cell cycle arrest. It effectively reverses cancer stemness and overcomes drug resistance in integrin β3 KRAS-dependent human pancreatic cancer stem cells, demonstrating significant tumor growth inhibition in orthotopic xenograft mouse models.
  5. Solasodine (also known as Purapuridine) is a steroidal alkaloid found in plants of the Solanaceae family. It induces apoptosis by inhibiting the p53–MDM2 complex and downregulating p21^Waf1/Cip1 and Bcl-2 proteins. Solasodine exhibits a range of biological activities, including neuroprotective, antifungal, hypotensive, anticancer, antiatherosclerotic, antiandrogenic, and anti-inflammatory effects.
  6. BRD4-p53 inhibitor

    SDU-071 is a potent, orally active inhibitor targeting the BRD4-p53 interaction. It inhibits the proliferation of MDA-MB-231 cells with an IC₅₀ of 10.5 μM and induces cell cycle arrest and apoptosis.
  7. MDM-2/p53 p53 Activator

    ReACp53 is a cell-penetrating peptide that inhibits p53 amyloid aggregation, restoring p53 function in cancer cell lines and organoids derived from high-grade serous ovarian carcinoma (HGSOC).
  8. p53 Activator

    DPBQ is a potent p53 activator that promotes apoptosis specifically in polyploid cells. It induces the expression and phosphorylation of p53 without inhibiting topoisomerase or directly binding to DNA. This selective action makes DPBQ a valuable tool for research involving polyploidy and the modulation of p53 signaling pathways.
  9. p53 Activator

    STIMA-1 is a p53 activator that stimulates mutant p53 DNA binding in vitro. This compound induces the expression of p53 target proteins and promotes apoptosis in human tumor cells expressing mutant p53. It serves as a valuable tool for researching p53-driven pathways and potential therapeutic strategies for cancers associated with p53 mutations.
  10. Anti-p53 Agent

    PK11007 is an anti-p53 agent that functions as a mild thiol alkylator, exhibiting significant anticancer activity. It selectively alkylates two surface-exposed cysteines on the p53 protein, leading to its stabilization without interfering with its DNA binding capabilities. Additionally, PK11007 promotes cell death in mutant p53 cancer cells by elevating reactive oxygen species (ROS) levels, making it a valuable compound for cancer research applications targeting p53 pathways.
  11. MDM-2/p53 MDM2 Inhibitor

    CTX1 is a selective inhibitor of MDM2, designed to alleviate HdmX-mediated repression of the tumor suppressor protein p53. This compound demonstrates significant anti-cancer activity, particularly in mouse models of acute myeloid leukemia (AML). CTX1 is utilized in research focused on cancer therapeutics and the modulation of p53 pathways.
  12. MDM-2/p53 MDM2 Inhibitor

    p53 and MDM2 proteins-interaction-inhibitor dihydrochloride is a selective inhibitor of the interaction between the tumor suppressor protein p53 and its negative regulator MDM2. This compound enhances p53 activity, highlighting its potential as an anticancer agent by promoting apoptosis in p53-deficient tumors. It is valuable for research applications focused on cancer therapy, cell cycle regulation, and the molecular mechanisms of tumorigenesis.
  13. p53-MDM2/X Inhibitor

    p53-MDM2-IN-4 is a potent inhibitor of the p53-MDM2/X protein interaction, displaying a Ki value of 3.079 μM. This compound effectively disrupts the MDM2-mediated inhibition of p53, promoting the stabilization and activation of the tumor suppressor protein. p53-MDM2-IN-4 holds significant potential in anti-tumor research and therapeutic development targeting cancer's reliance on the p53 pathway.
  14. p53-MDM2/X Inhibitor

    p53-MDM2-IN-1 is an inhibitor of the p53-MDM2/X protein interaction, exhibiting a Ki value of 23.35 µM. This compound is valuable for anti-tumor research, as it disrupts the interaction between p53 and MDM2/X, potentially restoring p53 function in cancer cells. Its application can enhance the understanding of tumor biology and contribute to the development of novel therapeutic strategies targeting this pathway.
  15. MDM-2/p53 MDM2 Inhibitor

    NVP-CGM097 sulfate is a selective inhibitor of the MDM2-p53 interaction, demonstrating an IC50 of 1.7±0.1 nM for human MDM2. This compound effectively disrupts the MDM2-mediated suppression of p53, leading to the activation of p53-dependent pathways. NVP-CGM097 sulfate is utilized in research focused on cancer therapeutics and the modulation of tumor suppressor activities.
  16. p53 Ubiquitination Inhibitor

    Hdm2 E3 ligase inhibitor 1 is a reversible inhibitor targeting the Hdm2 E3 ubiquitin ligase, which regulates the ubiquitination of the p53 tumor suppressor protein. With an IC50 value of 12.7 μM, this compound effectively inhibits the transfer of ubiquitin from preligated Ub-Ubc4 to p53, resulting in the stabilization of p53 protein levels within tumor cells. Its role in preventing p53 ubiquitination positions Hdm2 E3 ligase inhibitor 1 as a valuable tool for research in cancer biology and therapeutic development.
  17. p53-MDM2 Binding Inhibitor

    NU-8231 is a potent inhibitor of the p53-MDM2 interaction, exhibiting an IC50 range of 5.3-200 μM. This compound is instrumental in cancer research, facilitating studies on the restoration of p53 function and the modulation of apoptotic pathways. Its ability to disrupt the p53-MDM2 binding offers potential insights into therapeutic strategies targeting p53-mediated tumor suppression.
  18. MDM-2/p53 MDM2 Inhibitor

    AM-8735 is a selective inhibitor of the MDM2 protein, targeting its interaction with the p53 tumor suppressor. It exhibits potent activity with an IC50 of 25 nM, making it a valuable tool for cancer research. This compound is utilized in studies investigating the reactivation of p53 in tumor models, offering potential insights into therapeutic strategies for p53-deficient cancers.
  19. p53 Activator

    Tenovin-6 Hydrochloride is a p53 activator that enhances the transcriptional activity of the p53 tumor suppressor protein. This compound functions as a potent inhibitor of the protein deacetylase activities of human SIRT1, SIRT2, and SIRT3, with IC50 values of 21 μM, 10 μM, and 67 μM, respectively. Additionally, Tenovin-6 Hydrochloride inhibits dihydroorotate dehydrogenase (DHODH), making it valuable for research into cancer biology, cellular stress responses, and metabolic regulation.
  20. P53 Ligand

    Rezatapopt (PC14586) is a small-molecule ligand that specifically targets the mutated TP53 protein, particularly the Y220C variant. By binding to a unique pocket formed by this mutation, Rezatapopt restores the structural integrity and tumor suppressor functions of p53. This compound has shown promising antitumor activity, leading to tumor inhibition and regression in mouse models with established human tumor xenografts featuring the TP53 Y220C mutation, making it a valuable tool for cancer research targeting p53 dysfunction.
  21. p53 Inhibitor

    Pifithrin-α, p-Nitro, Cyclic is a potent p53 inhibitor that acts by blocking posttranscriptional activity of the p53 protein. This compound exhibits enhanced neuroprotective effects, demonstrating superior activity compared to traditional Pifithrin-α, particularly in cortical neurons exposed to Etoposide, with an ED50 of 30 nM. Importantly, Pifithrin-α, p-Nitro, Cyclic does not inhibit phosphorylation of p53 at the S15 residue, making it a valuable tool in studies of p53-related signaling pathways and neuroprotection research.
  22. P53 Activator

    SCH529074 is a potent p53 activator that selectively binds to the DNA binding domain (DBD) of p53 in a conformation-dependent manner, exhibiting a Ki of 1-2 μM. By restoring the function of mutant p53 and inhibiting HDM2-mediated ubiquitination of wild-type p53, SCH529074 offers valuable insights into p53 signaling pathways. This compound is particularly relevant for research focused on non-small-cell lung carcinoma (NSCLC) and other conditions associated with p53 dysfunction.
  23. Radioprotector/p53 Activator

    Amifostine thiol, an active metabolite of the cytoprotector Amifostine, serves as a radioprotector and p53 activator. This compound exerts cytoprotective properties by activating p53 via a JNK-dependent signaling pathway. Its biological activity makes Amifostine thiol suitable for research applications involving radiation protection and the study of p53-mediated cellular responses.
  24. p53 Y220C Activator

    p53 Activator 7 is a specialized activator for the p53 mutation Y220C, targeting the MDM2-p53 interaction with an EC50 of 104 nM. This compound enhances the DNA-binding capability of the mutant p53, offering valuable insight into p53 functionality and regulation. Additionally, p53 Activator 7 features a reactive alkyne group, enabling its use as a click chemistry reagent for copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. This characteristic expands its utility in chemical biology and molecular research applications.
  25. p53 Reactivator

    P53R3 is a potent p53 reactivator that restores sequence-specific DNA binding in p53 hotspot mutants, including p53R175H, p53R248W, and p53R273H. It induces p53-dependent antiproliferative effects with greater specificity than other compounds. P53R3 enhances the recruitment of both wild-type p53 and the p53M237I variant to various target gene promoters, and it significantly increases the mRNA, total protein, and cell surface expression of the death receptor 5 (DR5). This reagent is utilized in cancer research to explore the therapeutic potential of p53 reactivation.
  26. p53-Snail Binding Inhibitor

    GN25 is a selective inhibitor of the p53-Snail protein interaction, which plays a critical role in tumorigenesis. This compound exhibits antitumor activity by disrupting the binding of these proteins, potentially leading to the restoration of p53 tumor suppressor function. GN25 is suited for research applications aimed at exploring p53 signaling pathways and evaluating therapeutic strategies for cancer treatment.
  27. p53-Y220C Stabilizer

    MB710 is an aminobenzothiazole derivative that functions as a stabilizer for the oncogenic p53 mutation Y220C. By tightly binding to the Y220C pocket with a Kd of 4.1 μM, MB710 effectively stabilizes the p53-Y220C variant. This compound demonstrates significant anticancer activity in cell lines expressing the p53-Y220C mutation, making it a valuable tool for research in cancer biology and therapeutic development.
  28. p53 siRNA

    Teprasiran sodium is a small interfering RNA (siRNA) that specifically inhibits p53 activity, modulating p53-mediated apoptotic pathways. This reagent is vital for studying the cellular response to stress and mechanisms involved in acute kidney injury (AKI). Teprasiran sodium facilitates research into potential therapeutic strategies for AKI by temporarily blocking p53-related cell death.
  29. P53 Activating Peptide

    PK7088 is a pyrazole-based compound that serves as a specific p53 activating peptide. It facilitates the reactivation of mutant p53, restoring its wild-type functionalities. Due to its ability to enhance p53 activity, PK7088 demonstrates significant anticancer properties, making it a valuable tool in cancer research aimed at targeting p53 mutations.
  30. MDM2-p53 Inhibitor

    MDM2-p53-IN-16 is an inhibitor of the MDM2-p53 complex, demonstrating an IC50 value of 4.3 nM for the dissociation of the human p53/MDM2 interaction. By reactivating p53, it promotes apoptosis and cell-cycle arrest in Glioblastoma Multiforme (GBM) cells. This compound is suitable for use in cancer research, particularly in studies targeting p53 signaling pathways and therapeutic strategies for GBM.
  31. P53 Modulator

    Mutant p53 modulator-1 is a targeted modulator of mutant p53 protein. It exhibits potential to inhibit the progression of cancers harboring p53 mutations, making it a valuable tool for cancer research. This compound may aid in the development of therapeutic strategies aimed at restoring p53 function in tumor cells, thereby providing insights into the treatment of p53-related malignancies.
  32. p53 siRNA

    Teprasiran (QPI-1002) is a small interfering RNA that targets p53, a critical regulator of apoptosis. By temporarily inhibiting p53-mediated cell death, Teprasiran is primarily utilized in research to investigate mechanisms underlying acute kidney injury (AKI). Its ability to modulate cellular responses to stress makes it a valuable tool for studies focused on kidney pathology and potential therapeutic interventions.
  33. MDM-2/p53 Modulator

    PK9327 is a small-molecule modulator that targets the MDM2-p53 interaction, specifically stabilizing mutant p53 proteins that harbor cavity-creating mutations. By enhancing the stability of these mutant forms, PK9327 has the potential to restore p53 functionality and promote apoptotic signaling in cancer cells. This reagent is valuable for research applications focused on cancer therapeutics and the exploration of p53 pathway dynamics in malignancies.
  34. p53 Activator

    SLMP53-1 is a potent activator of both wild-type and mutant p53, demonstrating significant antitumor activity. This compound effectively reprograms glucose metabolism in cancer cells and inhibits angiogenesis, leading to a reduction in endothelial cell tube formation and vascular endothelial growth factor (VEGF) expression levels. SLMP53-1 is a valuable tool for research applications focused on cancer biology and therapeutic development targeting p53 pathways.
  35. p53 Mutant Stabilizer

    PK095 is a p53 mutant stabilizer that enhances the stability and function of mutated forms of the p53 protein. This compound is primarily utilized in cancer research, where it aids in the investigation of p53-related pathways and mechanisms of tumorigenesis. Its ability to stabilize p53 mutants makes it a valuable tool for studying therapeutic strategies targeting p53 abnormalities in various cancer models.
  36. MDM-2/p53 Inhibitor

    MX69-102 is an MDM-2/p53 inhibitor that promotes the degradation of MDM2, leading to the activation of the tumor suppressor p53 and subsequent apoptosis in cancer cells. This compound demonstrates significant efficacy in inhibiting xenografted human acute lymphoblastic leukemia (ALL) characterized by MDM2 overexpression in SCID mice, making it a valuable tool for cancer research and therapeutic development targeting the MDM2/p53 pathway.
  37. MDM-2/p53 Inhibitor

    Siremadlin (R Enantiomer) is a highly specific inhibitor of the MDM-2/p53 interaction. This compound exhibits potent biological activity in disrupting the MDM-2-mediated degradation of p53, thereby promoting p53-dependent tumor suppression. Siremadlin is valuable for research applications in cancer therapy, particularly in studies focused on restoring p53 function in tumor cells.
  38. p53 Activator

    NSC 66811 is a potent p53 activator that functions by inhibiting the interaction between MDM2 and p53, exhibiting a Ki of 120 nM for MDM2 binding. This compound reactivates p53, promoting its tumor suppressive functions, making it valuable for research in cancer biology, particularly in studies focused on MDM2-related pathways and p53 restoration. NSC 66811 is an essential tool for exploring therapeutic strategies aimed at overcoming MDM2-mediated p53 degradation in various malignancies.
  39. p53 Inhibitor

    NSC405640 is a potent inhibitor of the MDM2-p53 interaction, targeting the regulation of the p53 tumor suppressor protein. This compound effectively rescues structural mutations in p53, allowing for the restoration of its function. NSC405640 selectively inhibits the growth of cell lines expressing wild-type p53, making it a valuable tool for studying p53-related pathways and potential therapeutic applications in cancer research.
  40. p53 Activator

    p53 Activator 5 (compound 134A) is a robust activator of the p53 tumor suppressor protein, exhibiting a SC150 value of <0.05 mM. This compound effectively binds to mutant forms of p53, restoring their DNA-binding capability and demonstrating significant anti-tumor activity. Additionally, p53 Activator 5 serves as a click chemistry reagent, featuring an alkyne group that allows for copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, facilitating various research applications in molecular biology and cancer therapeutics.
  41. p53 Activator

    p53 Activator 3 (compound 87A) is a potent activator of the p53 tumor suppressor protein, demonstrating a SC150 value of less than 0.05 mM. This compound binds to mutant forms of p53, effectively restoring their DNA-binding capability and exhibiting significant anti-tumor activity. Additionally, p53 Activator 3 serves as a click chemistry reagent, featuring an alkyne group that enables copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions with azide-containing molecules, facilitating diverse biological applications.
  42. TP53 Oligonucleotide

    Cenersen is an oligonucleotide that specifically targets TP53. It effectively inhibits the activity of gain-of-function mutants of TP53, thereby enhancing the sensitivity of lymphoma cells to cytotoxic chemotherapy in vitro. This reagent is particularly valuable for research applications focused on chronic lymphocytic leukemia (CLL).
  43. HDM2-p53 Inhibitor

    MK-4688 is a potent inhibitor of the HDM2-p53 protein-protein interaction. By disrupting this interaction, MK-4688 plays a crucial role in restoring p53 function, which is often compromised in cancer cells. This compound is valuable for research applications focused on cancer biology, particularly in studies investigating p53 restoration and its implications in tumor suppression.
  44. p53 Activator

    MI 63 is a potent p53 activator that functions by inhibiting the MDM2 protein with a Ki of 3 nM. This compound effectively reduces the proliferation of embryonic rhabdomyosarcoma (ERMS) and alveolar rhabdomyosarcoma (ARMS) cells, demonstrating an IC50 value of 0.58 μM in RH36 cells. Additionally, MI 63 promotes apoptosis in both ERMS and ARMS, making it a valuable tool for research in cancer biology and therapeutic development targeting p53 pathways.
  45. MDM2-p53 Inhibitor

    AM-7209 is a potent and selective inhibitor of the MDM2-p53 interaction, exhibiting a dissociation constant (Kd) of 38 pM. It demonstrates significant inhibitory efficacy in the MDM2-amplified SJSA-1 osteosarcoma cell line with an IC50 of 1.6 nM. AM-7209 is primarily utilized in cancer research for its antitumor properties, specifically in studies aimed at reactivating p53 function in malignancies where MDM2 is overexpressed.
  46. MDM2-p53 Inhibitor

    ISA 27 is a small-molecule inhibitor of the MDM2-p53 protein-protein interaction. It effectively inhibits MDM2-mediated ubiquitination and degradation of p53, thereby stabilizing p53 levels. This compound is valuable for research on p53-mutant solid tumors, including thyroid and breast cancers, and offers a potential therapeutic strategy for targeting aberrant p53 signaling pathways.
  47. p53 Activator

    p53 Activator 12 is a potent activator of the p53 tumor suppressor protein, specifically designed to target mutant forms of p53. This compound effectively binds to mutated p53, restoring its capacity for DNA binding and transcriptional activity. p53 Activator 12 has significant potential in the research of cancer therapy, particularly in restoring the function of dysfunctional p53 in various tumors.
  48. MDM2-p53 Inhibitor

    MI-888 TFA is a potent MDM2-p53 interaction inhibitor with a Ki of 0.44 nM, demonstrating notable efficacy in disrupting the MDM2-p53 complex. This compound exhibits rapid, complete, and sustained tumor regression in xenograft mouse models, making it a valuable tool in cancer research. MI-888 TFA is suitable for studies investigating the modulation of p53 pathways and its potential therapeutic applications in oncology.
  49. p53 Activator

    p53 Activator 10 is designed to specifically activate the Y220C mutant form of the p53 tumor suppressor protein. By enhancing p53 activity, this compound plays a crucial role in promoting cell cycle arrest and apoptosis in cancer cells. It is primarily utilized in research focused on understanding the mechanisms of tumor suppression and therapeutic strategies against p53-related malignancies.
  50. MDM-2/p53 Interaction Inhibitor

    UNP-6457 is a potent inhibitor of the MDM2/p53 interaction, exhibiting an IC50 value of 8.9 nM. This compound plays a crucial role in disrupting oncogenic pathways by stabilizing the p53 tumor suppressor protein, leading to enhanced apoptosis in cancer cells. UNP-6457 is primarily utilized in cancer research to investigate the modulation of p53 activity and evaluate potential therapeutic strategies targeting the MDM2/p53 axis.

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