Apoptosis

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  1. 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.
  2. 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.
  3. 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.
  4. 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.
  5. 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.
  6. 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.
  7. 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.
  8. 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.
  9. 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.
  10. 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.
  11. 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.
  12. 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.
  13. 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.
  14. 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.
  15. 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.
  16. 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.
  17. 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.
  18. 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.
  19. 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.
  20. 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.
  21. 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).
  22. 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.
  23. 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.
  24. 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.
  25. 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.
  26. 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.
  27. 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.
  28. 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.
  29. 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.
  30. 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.
  31. 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.
  32. 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.
  33. 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.
  34. 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.
  35. ROCK Inhibitor

    3′-O-Demethyl-4′-N-demethyl-4′-N-acetyl-4′-epi-staurosporine is a selective inhibitor of Rho-associated protein kinase (ROCK), exhibiting IC50 values of 0.092 μM for PKC-α, 0.26 μM for ROCK, and 0.77 μM for ASK1. This compound demonstrates significant cytotoxic activity against human prostate cancer PC-3 cells, with an IC50 value of 0.16 μM. Its efficacy in inhibiting kinase activity makes it a valuable tool for research in cancer therapeutics and related signaling pathways.
  36. Caspase-3/Caspase-7 Inhibitor

    Ac-ESMD-CHO is an inhibitor of caspase-3 and caspase-7, targeting the proteolytic cleavage of the caspase-3 precursor peptide (CPP32) at the Glu-Ser-Met-Asp (ESMD) site. This compound is crucial for studying apoptosis and cellular signaling mechanisms by selectively modulating caspase activity. Its application extends to research areas involving cell death regulation and disease models where caspase-mediated pathways play a pivotal role.
  37. Glutathione Peroxidase Inhibitor

    4-Methylesculetin is a coumarin derivative that functions as a potent inhibitor of glutathione peroxidase. This compound exhibits significant antioxidant and anti-inflammatory properties, effectively inhibiting myeloperoxidase activity. In research applications, 4-Methylesculetin demonstrates the ability to attenuate bone resorption by downregulating elevated levels of bone-related exoglycosidases, cathepsin D, and tartrate-resistant acid phosphatases. Additionally, it reduces the expression of pro-inflammatory markers such as TNF-α, IL-1β, IL-6, COX-2, and PGE2, making it a valuable tool for studying inflammatory diseases.
  38. MDM2 Inhibitor

    D-CopA3 functions as an MDM2 inhibitor, promoting the activation of the p53 signaling pathway. It demonstrates significant cytotoxicity against colorectal cancer cell lines HCT-116, LoVo, and RKO, with an IC50 ranging from 15 to 18 μM, and induces JNK/Beclin-1-mediated autophagy. Additionally, D-CopA3 reduces the expression of the cell cycle inhibitor p21Cip1/Waf1, enhances mucosal barrier function, and exhibits anti-inflammatory properties in models of acute enteritis and chronic colitis. Furthermore, it has shown anti-tumor efficacy in HCT-116 mouse xenograft models.
  39. 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.
  40. PROTAC GPX4 Degrader

    PROTAC GPX4 degrader-5 is a selective degrader targeting GPX4, with a DC50 of 28 nM. This compound effectively induces ferroptosis and enhances reactive oxygen species (ROS) levels while exhibiting low toxicity to normal cells. PROTAC GPX4 degrader-5 demonstrates significant anti-proliferative effects in various tumor cell lines, making it a valuable tool for cancer research.
  41. Apoptosis Inducer

    Artocarpin is a potent apoptosis inducer that targets various signaling molecules, including NF-κB, Erk1/2, p38 MAPK, and Akt kinases. It stimulates the production of reactive oxygen species (ROS) and activates both p53-dependent and independent apoptotic pathways, resulting in G1-phase cell cycle arrest and autophagic cell death. Artocarpin displays significant cytotoxic and bactericidal effects against cancer cells, reduces bacterial burden, and possesses anti-inflammatory, analgesic, and anti-angiogenic properties, making it valuable for cancer and inflammatory research applications.
  42. PERK Inhibitor

    AMG PERK 44 is a highly selective inhibitor of the protein kinase PERK, exhibiting an IC50 of 6 nM. It demonstrates significant selectivity, being 1000-fold more potent than GCN2 (IC50 = 7300 nM) and 160-fold more selective over B-Raf (IC50 > 1000 nM). This compound has been shown to induce autophagy, making it a valuable tool for research into cellular stress responses and related metabolic pathways.
  43. 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.
  44. Apoptosis Inducer

    Kuanoniamine A is a pyridoacridine alkaloid that functions as an apoptosis inducer. Its primary mechanism involves the inhibition of DNA synthesis and regulation of the cell cycle, effectively decreasing the number of cells in the G2/M phase. Kuanoniamine A demonstrates significant anti-proliferative effects on human lymphocytes and is utilized in research focused on breast cancer, glioma, non-small cell lung cancer, and melanoma.
  45. ASK Inhibitor

    MSC 2032964A is a selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of 96 nM. This compound is shown to preserve visual responses in experimental autoimmune encephalomyelitis (EAE) mouse models and has significant efficacy in reducing neuroinflammation. Its application in research includes studies on neurodegenerative conditions and the modulation of inflammatory pathways.
  46. Pim/DAPK3 Inhibitor

    HS56 is an ATP-competitive dual inhibitor of Pim kinases and DAPK3, demonstrating Ki values of 0.26 μM for DAPK3, 0.208 μM for Pim-3, and over 100 μM for Pim-2 and Pim-1. This compound effectively inhibits LC20 phosphorylation and smooth muscle contraction, leading to a reduction in blood pressure in spontaneously hypertensive mouse models. HS56 is suitable for research investigating the mechanisms and potential treatments for hypertension.
  47. Apoptosis Inducer

    Tubulysin M is a potent apoptosis inducer that targets microtubules by inhibiting tubulin polymerization. This highly cytotoxic anti-microtubule agent exhibits exceptional activity against mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Its ability to induce cell cycle arrest and subsequent apoptosis makes Tubulysin M a valuable tool for research in cancer biology and drug resistance mechanisms.
  48. Apoptosis Inducer

    Tubulysin F is a potent apoptosis inducer that functions as an anti-microtubule toxin. Isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis, it exhibits strong cytotoxic activity across various mammalian cell types, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. By inhibiting microtubule and tubulin polymerization, Tubulysin F effectively leads to cell cycle arrest and subsequent apoptosis, making it a valuable reagent for research in cancer biology and drug resistance mechanisms.
  49. Apoptosis Inducer

    Tubulysin I is a potent apoptosis inducer that acts as an anti-microtubule toxin. Isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis, Tubulysin I exhibits significant cytotoxicity against mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. By inhibiting microtubule and tubulin polymerization, Tubulysin I disrupts cellular processes, leading to cell cycle arrest and subsequent apoptosis, making it a valuable tool for cancer research and studies on cell death mechanisms.
  50. Apoptosis Inducer

    Tubulysin G is a potent anti-microtubule toxin that targets microtubule dynamics by inhibiting tubulin polymerization. Derived from the myxobacteria Archangium geophyra and Angiococcus disciformis, Tubulysin G exhibits significant cytotoxicity towards mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Its ability to induce apoptosis and cause cell cycle arrest makes it a valuable reagent for research applications in cancer biology and cell death mechanisms.

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