Apoptosis

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  1. p53 Activator

    p53 Activator 14 is a potent activator of the p53 tumor suppressor pathway. This compound induces DNA damage, resulting in the activation of p53 and subsequent inhibition of proliferation in various cancer cell lines, with an IC50 of 7.21 μM in HCT116 cells. Additionally, it demonstrates the ability to inhibit cell adhesion, migration, and invasion, while also inducing cell cycle arrest and apoptosis. Its anti-angiogenic properties and antitumor efficacy have been validated using the chick chorioallantoic membrane (CAM) model, showcasing its potential for cancer research applications.
  2. Apoptosis Inducer

    TBP-134 is an apoptosis inducer that primarily targets the death receptor DR5, leading to G2/M phase cell cycle arrest. This compound is particularly relevant for research applications in pancreatic tumor studies, facilitating investigations into apoptotic pathways and therapeutic strategies. Its ability to selectively trigger apoptosis makes TBP-134 a valuable tool for cancer research.
  3. Anticancer Agent

    Tubulosine is an alkaloid that functions as a selective inhibitor of the Janus kinase 3 (JAK3) with an IC50 of 9.9 nM. It exhibits enhanced inhibition of JAK3 compared to other JAK family members, with IC50 values of 69.5 nM for JAK1, 84.9 nM for JAK2, and 76.3 nM for TYK2. Tubulosine induces both apoptotic and necrotic/autophagic cell death in cancer cells and disrupts peptide chain elongation in eukaryotic polysomes. This compound demonstrates promising anticancer activity, particularly in breast cancer cell lines, making it a valuable tool for cancer research.
  4. MDM2-p53 Interaction Inhibitor

    MI-773 TFA is a selective inhibitor of the MDM2-p53 interaction, demonstrating a Ki of 0.88 nM for MDM2. By disrupting the MDM2-TP53 interaction, MI-773 TFA effectively activates the p53 tumor suppressor pathway, leading to apoptotic cell death. This compound has shown significant anticancer activity, inducing tumor regression in xenograft models of adenoid cystic carcinoma and exhibiting therapeutic potential in neuroblastoma. MI-773 TFA serves as a valuable tool for research focused on p53-related cancer therapies.
  5. Apoptosis Inducer

    Galgravin is an apoptosis inducer derived from Nectandra megapotamica, exhibiting potent cytotoxic effects in vitro. This compound triggers programmed cell death in leukemia cells, making it a valuable tool for studying cancer biology and therapeutic applications. Its anti-inflammatory properties further emphasize its potential in cancer research and drug development.
  6. Apoptosis Inducer

    Anticancer agent 136 is a C17-triazole analogue of Geldanamycin that functions as an apoptosis inducer by targeting Hsp90. It demonstrates an IC50 of 3.38 μM in human dermal fibroblasts (HDF) and a dissociation constant (Kd) of 3.86 μM for Hsp90. This compound is useful for research investigating apoptosis pathways and the therapeutic potential of Hsp90 inhibition in cancer treatment.
  7. Apoptosis Inducer

    Antitumor agent-110 is an imidazotetrazine compound that functions as an apoptosis inducer primarily by arresting the cell cycle at the G2/M phase. This reagent exhibits favorable permeability properties and is suitable for applications in cancer research. Additionally, Antitumor agent-110 contains an alkyne functional group, facilitating its use in click chemistry via copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules.
  8. MDM2/MDMX Inhibitor

    MDMX/MDM2-IN-2 is a potent dual inhibitor of the p53-MDM2/MDMX interaction, exhibiting inhibition constants (Kis) of 0.23 µM for MDM2 and 2.45 µM for MDMX. This compound effectively disrupts the binding of p53 to MDM2 and MDMX, thereby restoring p53's function, which leads to cell cycle arrest and apoptosis. Additionally, MDMX/MDM2-IN-2 demonstrates inhibition of cell migration and invasion, highlighting its potential for therapeutic applications in cancer research. Its antitumor activity makes it a valuable tool for studying tumor biology and exploring novel cancer treatment strategies.
  9. Apoptosis Inducer

    [1,1′:4′,1′′-Terphenyl]-3,4′′,5-triol is an apoptosis inducer that targets cell cycle progression by blocking the transition from G0 to G1 phase. As a terphenyl derivative, it effectively induces differentiation in leukemia cells while exhibiting a strong apoptotic effect. This compound serves as a valuable tool in cancer research, particularly in studies focused on leukemia differentiation and apoptosis mechanisms.
  10. Apoptosis Inducer

    Lepidozin G is an apoptosis inducer that effectively inhibits the growth of various cancer cell lines, exhibiting IC50 values between 4.2 ± 0.2 and 5.7 ± 0.5 μM. This compound induces cell death in PC-3 prostate cancer cells through mechanisms related to mitochondrial apoptosis, making it a valuable tool for cancer research and drug development investigations focused on apoptosis pathways.
  11. Apoptosis Inducer

    MPI-0441138 is an apoptosis inducer that functions as a mitosis inhibitor. It promotes DNA breaks and facilitates the translocation of cytochrome c, which culminates in the death of tumor cells. This compound is valuable for research applications focused on cancer biology and therapeutic strategies aimed at inducing apoptosis in malignancies.
  12. Apoptosis Inducer

    IVHD-valtrate is a derivative of Valeriana jatamansi that functions as an apoptosis inducer. This compound has demonstrated efficacy against human ovarian cancer cells both in vitro and in vivo, promoting apoptosis and causing cell cycle arrest in the G2/M phase. IVHD-valtrate holds promise as a novel chemotherapeutic agent for research in ovarian cancer treatment.
  13. Apoptosis Inducer

    cpm-1285 is an apoptosis inducer that functionally inhibits intracellular Bcl-2 and related death antagonists. It demonstrates a strong binding affinity to Bcl-2, with an IC50 value of 130 nM. In preclinical studies, cpm-1285 effectively reduces tumor burden in murine models, making it a valuable tool for research on cancer therapies and the mechanisms of programmed cell death.
  14. Apoptosis Inducer

    MYRA-A is a potent apoptosis inducer that targets the Myc pathway. It functions by inhibiting Myc transactivation and interfering with the DNA-binding activity of Myc family proteins, leading to decreased cell viability. MYRA-A is valuable for research in cancer biology, particularly in studies related to Myc-driven malignancies and the mechanisms of apoptosis.
  15. NF-κB p65 Inhibitor, Apoptosis Inducer

    N-Desmethyldauricine is an inhibitor of NF-κB p65 with significant apoptotic effects. It effectively reduces p65 protein expression, induces apoptosis, and arrests the cell cycle at the G0/G1 phase. Additionally, N-Desmethyldauricine attenuates intercellular adhesion and inhibits the growth of 3D spheroids derived from triple-negative breast cancer. This compound is useful for research involving triple-negative breast cancer dynamics and therapeutic strategies.
  16. Apoptosis Inducer

    Antitumor agent-149 is an apoptosis inducer that functions by inhibiting HIF-1α-mediated transcription. This compound effectively promotes apoptosis in cancer cells, thereby contributing to the suppression of tumor growth. In preclinical studies, Antitumor agent-149 demonstrated significant efficacy in inhibiting tumor progression in the SW620 xenograft mouse model, making it a valuable tool for cancer research.
  17. Apoptosis Inducer

    Ganoderic acid Mf is a triterpenoid that acts as an apoptosis inducer, specifically targeting cancer cells. It promotes cell cycle arrest in the G1 phase, demonstrating significant selectivity for tumor versus normal cells. This compound induces apoptosis through a mitochondria-mediated pathway, making it a valuable reagent for cancer research and therapeutic studies.
  18. Apoptosis Inducer

    Sanguinarine (gluconate) is a benzophenanthridine alkaloid that functions as an apoptosis inducer. It promotes apoptosis through the generation of reactive oxygen species (ROS) and is linked to the activation of key signaling pathways, including JNK and NF-κB. This compound is utilized in research exploring mechanisms of apoptosis and oxidative stress responses in various cell types.
  19. Apoptosis Inducer

    Alpha-tocopheryloxyacetic acid (alpha-TEA) acts as an apoptosis inducer, specifically targeting pathways involved in programmed cell death. This compound demonstrates significant biological activity in promoting apoptosis in cancer cells, making it a valuable tool for research into both solid tumors and hematological malignancies. Its mechanism and application in oncological studies provide insights into potential therapeutic strategies for cancer treatment.
  20. Apoptosis Inducer

    Apoptosis Inducer 8 is a compound that acts as a galectin-1 (gal-1) mediated apoptosis inducer, specifically designed to target and initiate cell death in lung cancer cells. This reagent has demonstrated a significant reduction in gal-1 protein levels, contributing to its efficacy as an anti-cancer agent. Additionally, Apoptosis Inducer 8 serves as a positron emission tomography (PET) imaging agent, facilitating research applications in cancer diagnosis and therapy monitoring.
  21. Apoptosis Inducer

    Apoptosis Inducer 25 is a potent apoptosis inducer that specifically targets cell proliferation. It effectively inhibits the growth of BGC-823 cells with an IC50 of 0.37 μM, leading to cell cycle arrest in the G2/M phase. This compound further promotes apoptosis and triggers mitochondrial dysfunction, making it a valuable tool in cancer research. Its favorable pharmacokinetic profile in rat models underscores its potential for further investigation in therapeutic applications.
  22. p53 Inhibitor

    YL-1-9 is a potent inhibitor of p53 degradation mediated by MDM2, achieved through its strong binding to critical hydrophobic pockets within the MDM2 protein. This compound effectively induces cell cycle arrest and promotes apoptosis, particularly in breast cancer cells. YL-1-9 is valuable for research into p53-targeted therapies and the mechanisms of cancer cell proliferation and survival.
  23. Apoptosis Inducer

    Apoptosis Inducer 41 targets the mitochondrial pathway to trigger apoptosis in cancer cells. It displays potent inhibitory effects on MCF-7 cells, with an IC50 of 6.2 μM, and effectively induces cell cycle arrest in the G2/M phase. Additionally, Apoptosis Inducer 41 increases reactive oxygen species (ROS) accumulation and causes depolarization of the mitochondrial membrane potential. This compound is suitable for research focused on breast cancer and the mechanisms of programmed cell death.
  24. Apoptosis Inducer

    Apoptosis Inducer 36 is a potent apoptosis inducer targeting leukemia cells. It demonstrates significant anti-leukemic activity by reducing leukemia stem cells and promoting differentiation. This compound inhibits the proliferation of acute myeloid leukemia (AML) cells, causes cell cycle arrest at the G1 phase, and stimulates PANoptosis, encompassing apoptosis, pyroptosis, and necrosis. A prodrug form of Apoptosis Inducer 36 shows orally active antitumor efficacy in mouse models, making it a valuable tool for research in cancer therapeutics.
  25. Apoptosis Inducer

    Apoptosis Inducer 7 (Compound 5I) primarily targets apoptotic pathways to promote cell death in cancer cells. It activates the cleavage of PARP and caspases, while down-regulating the anti-apoptotic protein c-Flip and up-regulating the pro-apoptotic protein Noxa. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research focused on apoptosis mechanisms and therapeutic strategies.
  26. GP130 D1 domain inhibitor

    (R)-JAK2/STAT3-IN-1 is a selective inhibitor of the GP130 D1 domain, primarily targeting the JAK2/STAT3 signaling pathway. This compound demonstrates significant anti-tumor activity by inhibiting the phosphorylation of JAK2 and STAT3, thereby impairing tumor cell viability and migration while promoting apoptosis. With an affinity of 3.8 μM for GP130, (R)-JAK2/STAT3-IN-1 serves as a valuable tool for research into cancer biology and therapeutic interventions.
  27. Apoptosis Inducer

    Mechercharmycin A is a potent apoptosis inducer derived from the marine bacterium Thermoactinomyces sp. YM3-251. This compound demonstrates significant cytotoxicity and has shown strong antitumor activity in various biological models. It is utilized in research applications focusing on cancer cell apoptosis and the exploration of novel therapeutic strategies for tumor treatment.
  28. Apoptosis Inducer

    Camellianin A, a potent apoptosis inducer, primarily targets cancer cell proliferation. Derived from the leaves of A. nitida, it exhibits significant anticancer activity, particularly in human Hep G2 and MCF-7 cell lines. Additionally, Camellianin A demonstrates angiotensin-converting enzyme (ACE) inhibitory effects, making it relevant for research in cancer therapy and cardiovascular studies.
  29. Apoptosis Inducer

    Apoptosis Inducer 40 is a potent apoptosis inducer that primarily targets programmed cell death mechanisms. It demonstrates significant cytotoxic activity against Jurkat and NB4 cells, with IC50 values of 4.5 μM and 3.6 μM, respectively. By promoting apoptosis and cell cycle arrest, Apoptosis Inducer 40 is valuable for cancer research, particularly in studies focused on acute myeloid leukemia (AML).
  30. Apoptosis Inducer

    Bax BH3 peptide (55-74), wild type is a 20-amino acid peptide derived from the BH3 domain of Bax, a pro-apoptotic protein that promotes cell death through mitochondrial pathway activation. This peptide is effective in inducing apoptosis across various cell line models and serves as a valuable tool for studying apoptosis mechanisms and the role of BH3-only proteins in cellular processes. Researchers can utilize this peptide for investigations into cancer therapeutics and programmed cell death pathways.
  31. Apoptosis Inducer

    Antitumor agent-92 is an Icaritin derivative that functions as an apoptosis inducer. It effectively induces cell cycle arrest at the G0/G1 phase, leading to programmed cell death. This compound has significant potential for research applications in hepatocellular carcinoma (HCC) studies, providing a valuable tool for investigations into novel cancer therapies.
  32. Apoptosis Inducer

    Anticancer agent 153 functions as an apoptosis inducer through the generation of reactive oxygen species (ROS). This compound disrupts mitochondrial membrane potential (MMP), leading to the initiation of programmed cell death and effectively inhibiting cancer cell proliferation. Anticancer agent 153 is a valuable tool for research applications focused on understanding apoptosis mechanisms and evaluating potential therapeutic strategies against cancer.
  33. ASK Inhibitor

    ASK1-IN-6 is a selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of 7 nM in biochemical assays and 25 nM in cellular assays. This compound demonstrates potent anti-inflammatory properties and penetrates the blood-brain barrier, making it a valuable tool for studying neurodegenerative diseases, including Alzheimer's disease. Its specificity and efficacy position ASK1-IN-6 as a potential candidate for therapeutic exploration in related research applications.
  34. RET/BRAF/S6K/Src Inhibitor

    AD57 is an orally active multikinase inhibitor that targets RET, BRAF, S6K, and Src, effectively reducing mTOR activity. This compound demonstrates significant biological activity by interfering with critical signaling pathways involved in cancer proliferation and survival. AD57 is suitable for research applications focused on cancer biology and therapeutic development against malignancies driven by these kinases.
  35. RET/BRAF/S6K/Src Inhibitor

    AD57 hydrochloride is a multikinase inhibitor that targets RET, BRAF, S6K, and Src pathways. This orally active compound demonstrates significant biological activity in modulating aberrant signaling pathways associated with various cancers. Research applications include studying the effects of combined inhibition on tumor growth and resistance mechanisms in cancer cell lines and animal models.
  36. p53 DNA-binding inhibitor

    NSC194598 is a p53 DNA-binding inhibitor that effectively disrupts the interaction between p53 and DNA, exhibiting an IC50 value of 180 nM for in vitro studies and a range of 2-40 μM for in vivo applications. This compound has been shown to interfere with the transcriptional activation of the mutated RET gene in human medullary thyroid carcinoma TT cells. NSC194598 is utilized in research investigating acute toxicity effects on normal tissues due to radiation and chemotherapy.
  37. RET Inhibitor

    RET-IN-4 is a potent and selective RET inhibitor that demonstrates oral bioavailability, with IC50 values of 1.29 nM, 1.97 nM, and 0.99 nM against wild-type RET, RET V804M, and RET M918T variants, respectively. This compound exhibits improved selectivity against kinases such as JAK2 (IC50 of 4.4 nM) and FLT3 (IC50 of 30.8 nM). RET-IN-4 is primarily utilized in cancer research, highlighting its potential for therapeutic applications in RET-driven malignancies.
  38. p53 Reactivator

    Roslin 2 bromide, also known as Benzylhexamethylenetetramine bromide, is a reactivator of the p53 tumor suppressor protein. By binding to focal adhesion kinase (FAK), Roslin 2 bromide disrupts the interaction between FAK and p53, thereby enhancing p53 activity and exhibiting potential anticancer effects. This compound is suitable for research applications focused on cancer biology and the modulation of p53 signaling pathways.
  39. RET Inhibitor

    RET-IN-14 is a highly selective RET inhibitor that demonstrates potent inhibition with IC50 values of less than 0.51 nM for wild-type RET and varying nanomolar activity against RET mutations (G810R and V804M) as well as BTK and its C481S mutant. Its exceptional efficacy positions RET-IN-14 as a valuable tool for investigating RET-driven tumors and exploring therapeutic strategies in cancer research.
  40. c-KIT/PDGFR/RET Inhibitor

    KBP-7018 is a selective tyrosine kinase inhibitor targeting c-KIT, PDGFR, and RET. It demonstrates potent inhibition with IC50 values of 10 nM for c-KIT, 7.6 nM for PDGFR, and 25 nM for RET. This compound is valuable for investigating the molecular mechanisms and potential treatments related to idiopathic pulmonary fibrosis.
  41. c-KIT/PDGFR/RET Inhibitor

    KBP-7018 hydrochloride is a selective inhibitor of tyrosine kinases, specifically targeting c-KIT, PDGFR, and RET. It exhibits significant inhibitory potency, with IC50 values of 10 nM, 7.6 nM, and 25 nM, respectively. This compound is utilized in research focused on idiopathic pulmonary fibrosis, facilitating investigations into pathways associated with this condition.
  42. Survivin Antagonist

    Shepherdin (79-87) is a peptidomimetic antagonist targeting the interaction between Heat Shock Protein 90 (Hsp90) and Survivin. This fragment, representing amino acids 79 to 87 of the full Shepherdin sequence, demonstrates significant anticancer activity by disrupting the chaperone function of Hsp90, leading to the destabilization of Survivin. It is primarily utilized in cancer research to explore mechanisms of apoptosis and investigate therapeutic strategies targeting cell survival pathways.
  43. Hsp70 Binder, Apoptosis Inducer

    EV206 is a selective binder to the N-terminal domain of Hsp70, functioning as an apoptosis inducer. It promotes the degradation of Hsp70 through the ubiquitin-proteasome pathway, leading to reduced protein stability and inhibition of cellular growth. EV206 effectively induces apoptotic cell death in non-small cell lung cancer cells, suppresses colony formation, and downregulates markers associated with cancer stem cells. Additionally, it demonstrates anti-tumor activity in H460 xenograft models. This compound serves as a valuable tool for research in non-small cell lung cancer.
  44. Apoptosis Inducer

    Andrographolide is an interesting pharmacophore with anticancer and immunomodulatory activities and hence has the potential for being developed as a cancer therapeutic agent.
  45. Flunisolide is a corticosteroid often used to treat allergic rhinitis.The principal mechanism of action of Flunisolide is to activate glucocorticoid receptors, meaning it has an anti-inflammatory action.
  46. nonsteroidal anti-inflammatory agent

    Flurbiprofen is a nonsteroidal anti-inflammatory agent (NSAIA) with antipyretic and analgesic activity.
  47. nitroimidazole antibiotic medication

    Metronidazole is a nitroimidazole antibiotic medication used particularly for anaerobic bacteria and protozoa.
  48. TNF-alpha inhibitor

    Pomalidomide is a derivative of thalidomide and acts as an immunomodulator.
  49. E3 ubiquitin ligase inhibitor

    Thalidomide can directly inhibit angiogenesis induced by bFGF or VEGF in vivo.
  50. Bcl-2 inhibitor

    TW-37, a small-molecule inhibitor of Bcl-2, inhibits cell growth and induces apoptosis in pancreatic cancer mediated through a novel pathway involving inactivation of Notch-1 and Jagged-1.

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