Apoptosis

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  1. GPX4 Inhibitor

    GPX4-IN-1 is a potent inhibitor of glutathione peroxidase 4 (GPX4), a critical enzyme involved in cellular redox regulation. This compound exhibits significant antiproliferative activity, making it a valuable tool in cancer research. GPX4-IN-1 can be utilized to investigate mechanisms of cancer cell survival and sensitivity to oxidative stress, providing insights into targeted therapies for malignancies.
  2. GPX4 Activator

    DEL-I25 is a potent activator of glutathione peroxidase 4 (GPX4), a critical enzyme involved in cellular antioxidant defense. This compound effectively protects cells from ferroptosis, a form of regulated cell death associated with oxidative stress. DEL-I25 is valuable in research applications focused on understanding ferroptosis mechanisms and developing therapeutic strategies for diseases related to oxidative damage.
  3. STIM1-TFR1 Protein Complex Inhibitor

    STIM1-TFR1-IN-1 is an inhibitor of the STIM1-transferrin receptor 1 (TFR1) protein complex, exhibiting a binding affinity (Kd) of 2.18 μM to the STIM1-CD protein. This compound effectively disrupts the STIM1-TFR1 interaction, thereby decreasing TFR1-mediated iron uptake while inhibiting ferroptosis, lipid peroxidation, and reactive oxygen species (ROS) production. STIM1-TFR1-IN-1 also enhances glutathione peroxidase 4 (GPX4) activity and improves the glutathione/oxidized glutathione ratio, promoting neuroprotective effects and mitigating brain injury. This reagent is particularly relevant for studies focusing on intracerebral hemorrhage.
  4. Glutathione Peroxidase Activator

    RC363 is a novel glutathione peroxidase (GPx) activator designed to enhance the levels and activity of GPx1. This compound demonstrates protective effects on mouse hippocampal cells and primary cortical neurons against glutamate-induced oxidative cell death, specifically ferroptosis. RC363 is valuable for research investigating oxidative stress and neuroprotection mechanisms.
  5. GPX4 Inhibitor

    GPX4-IN-8 is a selective inhibitor of Glutathione Peroxidase 4 (GPX4), a key enzyme involved in cellular redox homeostasis. This compound exhibits significant antiproliferative activity, making it a valuable tool for research focusing on oxidative stress, ferroptosis, and cancer biology. GPX4-IN-8 can effectively facilitate investigations into the role of GPX4 in various disease models and therapeutic contexts.
  6. GPX4 Inhibitor

    LOC1886 is a covalent inhibitor targeting glutathione peroxidase 4 (GPX4), crucial for regulating oxidative stress within cells. It exhibits robust biological activity that aids in the investigation of ferroptosis and related cell death pathways. This compound is particularly useful for research applications focused on cancer biology, neurodegenerative diseases, and the study of oxidative damage mechanisms.
  7. Survivin Inhibitor

    MX107 is a selective survivin inhibitor known for its potent efficacy in suppressing the proliferation of triple-negative breast cancer (TNBC) cells. By inducing the degradation of survivin and inhibitor-of-apoptosis proteins (IAPs), MX107 effectively inhibits nuclear factor κB (NF-κB) activation in response to DNA damage. This compound enhances the tumoricidal effects of genotoxic treatments when used in conjunction with chemotherapeutic agents, making it a valuable tool in cancer research and therapy development.
  8. MDM2/XIAP Inhibitor

    MDM2/XIAP-IN-1 is a potent inhibitor of both MDM2 and XIAP, exhibiting significant anti-cancer activity with an IC50 value of 0.3 μM. This compound is suitable for use in cancer research, facilitating studies aimed at dissecting the role of MDM2 and XIAP in tumor progression and survival. Its dual-targeting mechanism allows for exploration of therapeutic strategies that may enhance apoptosis in cancer cells.
  9. RIPK2 Inhibitor

    CSLP43 is a selective inhibitor of RIPK2, demonstrating an IC50 of 19.9 nM against human RIPK2. By binding to the ATP-binding pocket of RIPK2, CSLP43 disrupts its interaction with the BIR2 domain of XIAP and cIAP1, effectively inhibiting RIPK2 ubiquitination and regulating NOD1- and NOD2-dependent inflammatory signaling pathways, as well as NF-κB activation. This compound is particularly relevant for research investigating Crohn's disease, Blau syndrome, early-onset sarcoidosis, and early-onset inflammatory bowel disease, due to its selectivity for the NOD1/NOD2 signaling pathway without affecting RIPK1 or RIPK3 activity.
  10. 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.
  11. 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.
  12. 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.
  13. MDM2 Inhibitor

    SP-141 is a selective inhibitor of MDM2, a protein that regulates the p53 tumor suppressor pathway. By promoting MDM2 auto-ubiquitination and subsequent degradation, SP-141 enhances p53 activity, which can lead to increased cell cycle arrest and apoptosis. This compound is a valuable tool for investigating therapeutic strategies in pancreatic and breast cancer research.
  14. 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.
  15. 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.
  16. 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.
  17. MDM2 Ligand

    MDM2 Ligand 5 is a potent ligand targeting the MDM2 protein, known for its role in regulating p53 activity. This compound serves as a critical building block for the development of Proteolysis Targeting Chimeras (PROTACs), facilitating the selective degradation of MDM2 to enhance p53-mediated tumor suppression. MDM2 Ligand 5 is valuable for research applications focused on cancer therapeutics and the modulation of oncogenic pathways.
  18. 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.
  19. 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.
  20. 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.
  21. 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.
  22. 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.
  23. PROTAC MDM2 degrader

    YX-02-030 is a PROTAC MDM2 degrader that effectively inhibits the MDM2-p53 interaction with an IC50 value of 63 nM, as well as the VHL-HIF1α binding, with an IC50 of 1.35 μM. By binding to MDM2, it recruits the VHL E3 ubiquitin ligase, promoting MDM2 degradation. This compound is particularly relevant in researching therapeutic strategies against p53 mutant or deleted triple-negative breast cancer (TNBC) cells.
  24. 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.
  25. CDK2/MDM2 Inhibitor

    CDK2/MDM2-IN-1 is a potent dual inhibitor targeting both CDK2 and MDM2, exhibiting an IC50 value of 2.60 nM for CDK2. This compound demonstrates significant antitumor activity, making it a valuable tool for research in cancer biology and therapeutic development. Its ability to simultaneously inhibit key regulatory proteins positions it as a promising candidate for studies focused on cell cycle regulation and apoptosis.
  26. 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.
  27. 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.
  28. 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.
  29. 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.
  30. 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.
  31. 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.
  32. MDM2/MDMX Inhibitor

    ATSP-7041 is a selective dual inhibitor of MDM2 and MDMX, designed to reactivate the p53 tumor suppressor pathway. This compound demonstrates significant biological activity in p53-positive cancers, providing a potential therapeutic strategy for tumorigenesis associated with p53 pathway dysregulation. Research applications include studying the regulation of cancer cell apoptosis and the effects of p53 reactivation on tumor growth dynamics.
  33. 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.
  34. 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.
  35. 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.
  36. 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.
  37. 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).
  38. 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.
  39. MDM2 Inhibitor

    Milademetan tosylate is a potent inhibitor of MDM2, functioning through the restoration of p53 activity by disrupting the p53-MDM2 interaction. This compound effectively arrests the cell cycle in the G1 phase and induces apoptosis, demonstrating significant anticancer activity. Milademetan tosylate shows promise in research related to Merkel cell carcinoma (MCC) and other malignancies involving dysfunctional p53 signaling.
  40. 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.
  41. 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.
  42. 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.
  43. MDM2 Inhibitor

    MDM2-IN-21 is a potent inhibitor of the MDM2 protein, which plays a critical role in the regulation of the p53 tumor suppressor pathway. By disrupting the MDM2-p53 interaction, MDM2-IN-21 activates p53-dependent signaling, leading to enhanced apoptosis and cell cycle arrest in cancer cells. This compound is widely utilized in cancer research to explore therapeutic strategies targeting MDM2 and to investigate its role in tumorigenesis and cellular responses to stress.
  44. 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.
  45. MDM2/MDM4 Inhibitor

    RDR03871 is a potent dual inhibitor of MDM2 and MDM4, demonstrating IC50 values of 35.4 nM and 10.4 nM for the MDM2-p53 and MDM4-p53 interactions, respectively. This compound plays a significant role in cancer research by modulating p53 pathways, thus offering a potential therapeutic avenue for tumors with dysregulated MDM2/MDM4 signaling. RDR03871 is suitable for studies focused on the restoration of p53 function in malignancies.
  46. 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.
  47. 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.
  48. 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.
  49. mutant p53 (R175H) Activator, Metal Ion Chelator, Zinc Ionophore

    ZMC2 is a thiosemicarbazone-class metal ion chelator and zinc ionophore that specifically targets the mutant p53 protein (R175H) with a binding affinity (Ka) of 27.4 nM. This compound effectively facilitates the transport of zinc ions across cellular membranes and restores zinc binding to zinc-deficient p53 mutants, which can reinstate the wild-type structure and function necessary for site-specific DNA binding. Additionally, ZMC2 generates reactive oxygen species (ROS), making it a valuable tool for cancer research applications.
  50. MDM2-p53 Inhibitor

    BI-0282 is a potent inhibitor of the MDM2-p53 interaction. This compound disrupts the negative regulation of the p53 tumor suppressor by MDM2, thereby enhancing p53-mediated transcriptional activity. BI-0282 is primarily used in research applications focused on cancer therapy, specifically in studies aimed at restoring p53 function in tumor cells. Its ability to stabilize p53 makes it a valuable tool for exploring therapeutic strategies targeting MDM2 in various malignancies.

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