Apoptosis

Items 351-400 of 1195

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  1. ASK1 Inhibitor

    TC ASK 10 is a selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1), exhibiting an IC50 of 14 nM. This compound demonstrates minimal inhibitory activity against a range of other kinases, with ASK2 being the only exception, showing an IC50 of 0.51 μM. TC ASK 10 is valuable for research applications focused on apoptosis regulation and cellular stress response pathways.
  2. Granzyme B/Caspase-8 Inhibitor

    Ac-IETD-CHO is a potent, reversible inhibitor of granzyme B and caspase-8. By blocking these proteases, Ac-IETD-CHO effectively inhibits Fas-mediated apoptotic cell death, as well as preventing hemorrhage and liver failure. This compound is valuable for research in apoptosis, immune response, and the modulation of cytotoxic T lymphocyte-induced cell death.
  3. Apoptosis Inducer

    Lucidenic acid B is a natural compound derived from Ganoderma lucidum that serves as an apoptosis inducer. It stimulates the activation of caspase-9 and caspase-3, leading to the cleavage of PARP in cancer cells. Notably, Lucidenic acid B does not alter the cell cycle profile or increase the number of necrotic cells, making it a valuable reagent for research in cancer biology and apoptosis studies.
  4. Apoptosis Inducer

    Cantrixil, an active enantiomer of TRX-E-002, functions as a potent apoptosis inducer. It elevates phosphorylated c-Jun levels, leading to caspase-mediated apoptosis specifically in ovarian cancer cells. This second-generation super-benzopyran compound demonstrates significant pan anti-cancer activity across a variety of cancer phenotypes, making it a valuable tool for research into cancer therapeutics and mechanisms of cell death.
  5. MDM2 Inhibitor

    Milademetan tosylate hydrate is a selective, orally active inhibitor of MDM2, primarily utilized in research focused on acute myeloid leukemia (AML) and solid tumors. This compound induces G1 cell cycle arrest, promotes cellular senescence, and triggers apoptosis, making it a valuable tool for studying the therapeutic potential in cancer treatment and the underlying mechanisms of tumor biology.
  6. Apoptosis Inducer

    13'-Carboxy-δ-tocopherol, a metabolite of long-chain vitamin E, serves as an apoptosis inducer by activating caspase-3 and caspase-9, leading to PARP-1 cleavage. This compound demonstrates significant antiproliferative effects in cancer cells by reducing mitochondrial membrane potential and increasing reactive oxygen species (ROS) formation, ultimately driving apoptosis. 13'-Carboxy-δ-tocopherol is valuable in research focused on hepatocellular carcinoma and other cancer types.
  7. Mdm2-MdmX RING Domain Inhibitor

    MMRi6 is an Mdm2-MdmX RING domain inhibitor that disrupts the RING-RING interaction between Mdm2 and MdmX. This compound effectively inhibits MdmX-stimulated Mdm2 autoubiquitination and Mdm2-MdmX-mediated polyubiquitination of p53 in vitro, while sparing NEDD4-1 autoubiquitination. MMRi6 promotes stabilization and accumulation of p53, leading to PARP cleavage in wild-type p53 Emu-myc lymphoma cells. It demonstrates growth inhibition of wild-type p53 and p53-null Emu-myc lymphoma cells with IC50 values of approximately 0.5 μM and 3 μM, respectively, making it a valuable tool for studying leukemia and lymphoma.
  8. PKD Inhibitor

    BPKDi is a potent inhibitor of Protein Kinase D (PKD), targeting PKD1, PKD2, and PKD3 with IC50 values of 1 nM, 9 nM, and 1 nM, respectively. This compound effectively disrupts signal-dependent phosphorylation and nuclear export of class IIa histone deacetylases (HDACs) in cardiomyocytes, consequently attenuating cellular hypertrophy. BPKDi serves as a valuable tool for investigating the role of PKD in cardiovascular research and therapeutic interventions.
  9. PROTAC Glutathione Peroxidase Degrader

    NC-R17 is a non-covalent degrader targeting Glutathione Peroxidase 4 (GPX4) through the PROTAC mechanism, designed to induce ferroptosis in cancer cells. Exhibiting significant antitumor activity, NC-R17 facilitates the targeted degradation of GPX4, contributing to research in cancer biology and therapeutic strategies. The compound combines a Demethyl-RSL3 ligand for GPX4 with an E3 ubiquitin ligase ligand derived from Lenalidomide, connected by a specific PROTAC linker to enhance its biological activity.
  10. Ferroptosis/Apoptosis Inducer

    Lepadin H is a potent ferroptosis and apoptosis inducer, demonstrating significant in vitro cytotoxicity and in vivo antitumor efficacy against cancer cells. This compound functions by decreasing the levels of GPX4 and SLC7A11, while enhancing p53 and ACSL4 expression. Lepadin H promotes the generation of lipid hydroperoxides and increases reactive oxygen species (ROS), leading to a reduction in cellular glutathione (GSH) levels and lipid peroxidation. Additionally, it causes G2/M phase cell cycle arrest and inhibits the clonogenic growth and migration of melanoma cells, making it a valuable tool for cancer research.
  11. GPX4 Degrader

    GDCNF-11 is a potent HIM-PROTAC degrader targeting GPX4, utilizing the chaperone protein HSP90 to facilitate degradation. This compound promotes the ubiquitination of GPX4, leading to reduced expression levels, which in turn induces ferroptosis in HT-1080 cells. GDCNF-11 has a DC50 value of 0.08 μM, making it a valuable tool for studying ferroptosis and GPX4-related pathways in various biological research applications.
  12. GPX4 Targeting AUTAC

    GPX4-AUTAC is a GPX4-targeting autophagy-mediated degrader designed to selectively induce degradation of GPX4 through autophagy. By promoting the ubiquitination of GPX4 via E3 ligase TRAF6, it enhances the interaction with p62, facilitating the autophagy-dependent degradation process. GPX4-AUTAC has been shown to significantly induce ferroptosis and exhibit notable anti-cancer activity in breast cancer cells, breast cancer-derived organoids, and in the MDA-MB-231 tumor xenograft model. Additionally, it demonstrates potent synergistic effects when used in combination with drugs such as Sulfasalazine or traditional chemotherapy agents like Paclitaxel or Cisplatin.
  13. Glutathione Peroxidase Mimic

    Ebselen derivative 1 is a potent glutathione peroxidase (GPx) mimic with oral activity, designed to provide protective effects against oxidative damage. It exhibits significant protective capabilities against cisplatin-induced hair cell (HC) damage, effectively mitigating oxidative stress, apoptosis, and ferroptosis in hair cells. This compound serves as a valuable tool for research into cisplatin-induced hearing loss and related oxidative stress pathways.
  14. GPX4 Inhibitor

    GPX4-IN-11 is a potent inhibitor of GPX4, demonstrating a KD of 45.7 μM. This compound is significant in the study of ferroptosis, enabling researchers to investigate the mechanisms underlying oxidative stress and cell death. Its utility in various biological assays contributes to the understanding of GPX4's role in disease processes and potential therapeutic approaches.
  15. GPX4 Inhibitior

    GPX4-IN-18 is a ferrocene-containing inhibitor targeting glutathione peroxidase 4 (GPX4), recognized for its role in inducing ferroptosis. This compound significantly elevates reactive oxygen species (ROS) and malondialdehyde (MDA) levels in OS-RC-2 clear cell renal carcinoma cells, demonstrating potent biological activity. In HT-1080 cells, GPX4-IN-18 exhibits an IC50 of 0.007 μM in the absence of ferrostatin-1, and 1.486 μM when ferrostatin-1 is present. Additionally, GPX4-IN-18 has been shown to reduce tumor volume and intratumoral GPX4 levels in xenograft models, making it a valuable tool for researching ferroptosis-related pathways.
  16. GPX4 Inhibitor

    GPX4-IN-13 is a potent inhibitor of GPX4, targeting its role in cellular antioxidant defense mechanisms. This compound exhibits significant anticancer activity by promoting ferroptosis and reducing proliferation in thyroid cancer cells. It demonstrates inhibitory effects on the growth of various thyroid cancer cell lines, with IC50 values of 8.39 μM for N-thy-ori-3-1, 10.28 μM for MDA-T32, and 8.18 μM for MDA-T41. GPX4-IN-13 is instrumental for research in cancer biology and therapeutic development targeting GPX4-dependent pathways.
  17. GPX4 Inhibitor

    GPX4-IN-12 is a non-covalent inhibitor of Glutathione Peroxidase 4 (GPX4), primarily targeting this enzyme to induce ferroptosis. This compound effectively inhibits cell proliferation in HT1080 cells, making it a valuable tool for studying the mechanisms of ferroptosis and its implications in cancer research. GPX4-IN-12 is suitable for investigations into oxidative stress and related pathways within various biological contexts.
  18. GPX4 Inhibitor

    GPX4-IN-21 is a selective inhibitor of glutathione peroxidase 4 (GPX4), a key regulator in cellular redox homeostasis. This compound effectively induces ferroptosis by downregulating ferroptosis-related proteins, including SLC7A11, SLC11A2, and GPX4, leading to increased levels of reactive oxygen species (ROS) and malondialdehyde (MDA). GPX4-IN-21 demonstrates significant anti-proliferative activity and is useful for investigating therapeutic strategies in cancer research, particularly in models of melanoma.
  19. GPX4 Degrader

    GPX4 degrader-1 (Compound RS-1) is a hydrophobic tagging (HyT)-mediated degrader specifically targeting GPX4, exhibiting a DC50 value of 8.9 nM in HT1080 cells. This compound effectively induces GPX4 degradation, promoting ferroptosis through the accumulation of lipid reactive oxygen species (ROS). Additionally, GPX4 degrader-1 has shown significant antitumor efficacy in preclinical murine mammary carcinoma models, making it a valuable tool for cancer research and therapeutic study.
  20. GPX4 PROTAC Degrader

    PROTAC GPX4 degrader-4 selectively targets GPX4, functioning as a PROTAC degrader with a DC50 of 5.32 nM. This compound effectively inhibits the proliferation of RT4, T24, and J82 bladder cancer cell lines, exhibiting IC50 values of 0.09, 2.97, and 7.58 μM, respectively. PROTAC GPX4 degrader-4 promotes the accumulation of lipid reactive oxygen species (ROS) and triggers ferroptosis in T24 and RT4 cells. Additionally, it demonstrates significant antitumor efficacy in a T24 tumor-bearing BALB/c nude mouse model, making it a valuable tool for bladder cancer research.
  21. Apoptosis Inducer

    α-Eleostearic acid is a conjugated linolenic acid that functions as an apoptosis inducer, demonstrating its role in prompting programmed cell death. Additionally, it acts as a ferroptosis inducer, contributing to a unique mechanism of cell death associated with iron metabolism. This compound exhibits notable antioxidant properties and displays antitumor activity, making it a valuable reagent for research in cancer biology and cell death mechanisms.
  22. GPX4 Activator

    GPX4 Activator 1 is an allosteric modulator that targets GPX4, demonstrating a Kd of 5.86 μM and an EC50 of 19.19 μM. This compound effectively enhances GPX4 activity, thereby inhibiting ferroptosis by preventing the accumulation of intracellular lipid peroxides induced by ferroptosis inducers. It serves as a valuable tool for researchers studying ferroptosis mechanisms and potential therapeutic interventions in diseases associated with oxidative stress.
  23. GPX4 Inhibitor

    NPD4928 is a potent GPX4 inhibitor that enhances RSL3-dependent ferroptosis through its unique mechanism of action. By binding to ferroptosis suppressor protein 1 (FSP1), NPD4928 effectively inhibits its enzymatic activity, thereby promoting ferroptotic cell death. This compound is valuable for research applications focused on studying ferroptosis pathways and identifying potential therapeutic targets in cancer and neurodegenerative diseases.
  24. GPX4 Inhibitor

    GPX4-IN-6 is a covalent inhibitor of GPX4, exhibiting an IC50 of 0.13 μM. This compound effectively induces ferroptosis, making it a valuable tool for studying mechanisms related to triple-negative breast cancer (TNBC). Its role in modulating oxidative stress pathways presents significant implications for cancer research and therapeutic development.
  25. GPX4 Inhibitor

    JKE-1716 is a potent and selective inhibitor of glutathione peroxidase 4 (GPX4). It induces ferroptosis through the covalent modification of GPX4, making it a valuable tool for studying iron-dependent cell death mechanisms. This compound is applicable in research focusing on cancer biology, neurodegenerative diseases, and oxidative stress-related studies.
  26. GPX4 Inhibitor

    RSL3-NH2 is a selective inhibitor of GPX4, a crucial regulator of lipid peroxidation and ferroptosis. By promoting ferroptosis in cancer cells, RSL3-NH2 serves as an effective tool for studying cell death pathways and cancer metabolism. Additionally, this compound can be utilized as a cytotoxic payload in the development of antibody-drug conjugates (ADCs), enhancing targeted therapeutic strategies in cancer research.
  27. GPX4 Inhibitor

    GPX4-IN-9 is a selective inhibitor of glutathione peroxidase 4 (GPX4), effectively promoting ferroptosis under both in vitro and in vivo conditions. This compound demonstrates significant cytotoxic effects on pancreatic cancer cells, making it a valuable tool for cancer research. Its mechanisms of action offer insights into the role of GPX4 in cancer cell survival and potential therapeutic strategies targeting ferroptosis.
  28. GPX4 Inhibitor

    GPX4-IN-19 is a potent inhibitor of GPX4, exhibiting an IC50 of 0.311 μM through covalent binding to the Sec 46 site. This compound demonstrates significant anti-proliferative effects with a high selectivity for inducing ferroptosis, characterized by intracellular Fe2+ accumulation and elevated levels of lipid peroxides (LPOs) and reactive oxygen species (ROS). GPX4-IN-19 is particularly relevant for research in Triple-Negative Breast Cancer (TNBC), as it induces ferroptosis and subsequent DNA damage.
  29. YAP-GPX4 Signaling Modulator

    Pipecolic acid is a metabolite of lysine that acts as a YAP-GPX4 signaling modulator. It exhibits antioxidant properties and has been shown to reduce retinal vascular tube formation while mitigating ferroptosis. This compound enhances voltage-sensitive Ca2+ channel currents and can induce neuronal apoptosis, making it a valuable tool for research on diabetic retinopathy. Its ability to cross the blood-brain barrier further supports its application in neurological studies.
  30. Nrf2-Gpx4 Activator

    Gingerenone A is an Nrf2-Gpx4 activator that triggers ferroptosis in liver tissue, demonstrating significant potential for therapeutic intervention in liver damage. This compound exhibits notable anti-inflammatory, anti-diabetic, anti-tumor, and pro-aging properties observed in murine models, making it valuable for research in oxidative stress regulation and associated diseases. Its oral bioactivity further enhances its applicability in in vivo studies.
  31. GPX4 Inhibitor

    JKE-1674 is a potent inhibitor of glutathione peroxidase 4 (GPX4), functioning through modulation of cellular redox status. This orally active compound, an analog of ML-210 with a structural modification to the nitroisoxazole ring, demonstrates strong cytotoxicity against LOX-IMVI cells, akin to that of ML-210. Notably, cell viability is restored upon treatment with ferroptosis inhibitors, underscoring its utility in studying ferroptotic cell death pathways and oxidative stress in various biological contexts.
  32. GPX4 Inhibitor

    GPX4-IN-3 is a selective inhibitor of glutathione peroxidase 4 (GPX4), serving as a potent inducer of ferroptosis. At a concentration of 1 μM, GPX4-IN-3 demonstrates 71.7% inhibition of GPX4 activity. This compound is valuable for research applications focused on oxidative stress, cell death mechanisms, and potential therapeutic strategies against various cancers and neurodegenerative diseases.
  33. GPX4 Inhibitor

    GPX4-IN-5 is a potent covalent inhibitor of GPX4, exhibiting an IC50 of 0.12 μM. This compound induces ferroptosis, demonstrating significant anti-tumor activity. GPX4-IN-5 is particularly relevant for research applications focused on triple-negative breast cancer (TNBC).
  34. MDM2-MDM4 Inhibitor

    MMRi62 is an MDM2-MDM4 inhibitor that promotes ferroptosis by targeting negative regulators of the tumor suppressor p53. It exhibits P53-independent pro-apoptotic activity against pancreatic ductal adenocarcinoma (PDAC) cells and induces autophagy. MMRi62 augments reactive oxygen species levels and triggers lysosomal degradation of ferritin heavy chain (FTH1), while also facilitating the proteasomal degradation of mutant p53. Moreover, MMRi62 demonstrates efficacy in vivo by inhibiting orthotopic xenograft models of PDAC characterized by frequent KRAS and TP53 mutations, supporting its potential in cancer research applications.
  35. GPX4 Activator

    GPX4 Activator 2 is a potent activator of glutathione peroxidase 4 (GPX4), a key enzyme involved in reducing oxidative stress. It demonstrates significant cardioprotective effects and effectively inhibits cellular ferroptosis with an EC50 of 7.8 μM. This compound is valuable for research applications focused on myocardial injury and the mechanisms of ferroptosis in cardiovascular diseases.
  36. Apoptosis Inducer

    (-)-Alkannin is a potent apoptosis inducer, extracted from Alkanna tinctoria, and has demonstrated significant anticancer activity. It effectively arrests the cell cycle and triggers apoptotic processes in various cancer cell lines. Additionally, (-)-Alkannin contributes to the reduction of hepatic inflammation through modulation of the Rho-kinase pathway, making it a valuable tool for research in cancer biology and inflammation studies.
  37. Apoptosis Inducer

    Obacunone is a triterpenoid limonoid with potent apoptosis-inducing properties. It has demonstrated significant anticancer effects through the activation of programmed cell death pathways. Additionally, Obacunone offers protective benefits to retinal pigment epithelial (RPE) cells against oxidative damage caused by ultraviolet (UV) radiation, making it a valuable reagent for research in cancer biology and oxidative stress studies.
  38. Apoptosis Inducer

    Icaritin is a prenylflavonoid derivative that functions as an apoptosis inducer. It has demonstrated potent inhibitory effects on the proliferation of K562 cells, with an IC50 of 8 µM, and primary chronic myeloid leukemia (CML) cells, exhibiting IC50 values of 13.4 µM for CML-chronic phase and 18 µM for CML-blast crisis. Icaritin modulates critical signaling pathways, including MAPK/ERK/JNK and JAK2/STAT3/AKT, and has been shown to enhance osteogenesis, making it a valuable compound for research in cancer and regenerative medicine.
  39. Apoptosis Inducer

    Pimpinellin is an apoptosis inducer derived from Cyrtomium fortumei. It demonstrates significant antitumor activity by promoting apoptosis in tumor cells, thereby inhibiting cellular growth and proliferation. This compound has potential applications in cancer research, particularly in studies focused on mechanistic pathways of cell death and therapeutic strategies for tumor suppression.
  40. Apoptosis Inducer

    9-Methoxycamptothecin (MCPT) is a potent apoptosis inducer that exerts its antitumor effects primarily through the inhibition of topoisomerase enzymes. Derived from Camptotheca acuminata, MCPT effectively induces G2/M cell cycle arrest and promotes apoptosis in various cancer cell lines. This compound is valuable for research applications focused on understanding cancer biology and therapeutic strategies targeting apoptotic pathways.
  41. Apoptosis Inducer

    Linderalactone is a sesquiterpene lactone that acts as an apoptosis inducer by modulating the expression of apoptosis-related proteins and inhibiting the JAK/STAT signaling pathway. This compound has been shown to effectively inhibit the proliferation of lung cancer A-549 cells, displaying an IC50 of 15 µM. Its unique mechanism makes Linderalactone a valuable tool for research in cancer biology and therapeutic development.
  42. Apoptosis Inducer

    Melamine is an orally active apoptosis inducer that targets multiple biological pathways. It is effective in inducing disease models in animals, particularly concerning male reproductive function through its effects on Sertoli cells. Additionally, melamine exhibits neurotoxic and nephrotoxic properties, making it useful for research on cognitive impairment and acute kidney injury. Its potential to induce bladder cancer and urinary stone models further establishes melamine as a valuable tool in toxicological and cancer research.
  43. Apoptosis Inducer

    Bucladesine calcium is a cell-permeable analog of cyclic AMP (cAMP), functioning as an apoptosis inducer primarily through the activation of cAMP-dependent protein kinase (PKA). By elevating intracellular cAMP levels, it inhibits phosphodiesterase (PDE) activity, thereby stabilizing cAMP concentrations and promoting apoptosis in targeted cells. This compound is widely utilized in research applications investigating cell signaling pathways, PKA-mediated processes, and mechanisms underlying programmed cell death.
  44. 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.
  45. 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.
  46. 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.
  47. 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.
  48. 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.
  49. 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.
  50. 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.

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