Apoptosis

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  1. Caspase-6 Inhibitor

    ED11 is a selective inhibitor of caspase-6, demonstrating an IC50 of 12.12 nM. By competing with Huntingtin (Htt) for the active site of caspase-6, ED11 effectively reduces Htt cleavage. Notably, ED11 possesses the ability to cross the blood-brain barrier, making it a valuable reagent for research into Huntington's disease and related neurodegenerative disorders.
  2. Caspase-9 Inhibitor

    Z-LEHD-FMK TFA is a selective and irreversible inhibitor of caspase-9, primarily involved in the apoptosis pathway. This compound demonstrates significant neuroprotective effects, particularly in models of spinal cord injury, and has been shown to mitigate lethal reperfusion injury. It is a valuable tool for research focused on therapeutic strategies against apoptotic cell death and neuroprotection.
  3. Caspase Inhibitor

    Ac-DMQD-CHO is a selective inhibitor of caspase 3, exhibiting an IC50 of 39 nM. This compound effectively reduces apoptosis, making it a valuable tool in studies related to neuroprotection and cellular survival. Its application in research can aid in the exploration of therapeutic strategies targeting neurodegenerative diseases and apoptosis-related conditions.
  4. Caspase-8 Inhibitor

    Z-LE(OMe)TD(OMe)-FMK is a selective inhibitor of caspase-8, a key enzyme involved in the apoptotic pathway. By inhibiting caspase-8 activity, this reagent effectively prevents apoptosis in various cell types, making it a valuable tool for studying cell survival mechanisms. It is widely used in research applications focused on programmed cell death and related signaling pathways.
  5. Caspase-3 Inhibitor

    Ac-DMQD-AMC is a selective inhibitor of caspase-3, a critical executioner caspase in the apoptosis pathway. This compound features an aromatic amine structure and is synthesized using the aminium-based coupling reagent HATU alongside 2,4,6-trimethylpyridine (TMP). Ac-DMQD-AMC is suitable for research applications focused on studying apoptosis, cellular signaling, and the role of caspases in various diseases.
  6. Caspase-3 Inhibitor

    Ac-AAVALLPAVLLALLAP-DEVD-CHO is a specific and reversible inhibitor of caspase-3, a key executioner in the apoptotic pathway. This compound effectively reduces caspase-3 activity, making it a valuable tool for studying apoptosis and cell death mechanisms in various biological contexts. Its application extends to research on neurodegenerative diseases, cancer, and other conditions where caspase-3 plays a pivotal role in cellular regulation.
  7. Caspase-4 Inhibitor

    Ac-AAVALLPAVLLALLAP-LEVD-CHO is a cell-permeable inhibitor of caspase-4, a crucial mediator of inflammation and cell death pathways. This compound demonstrates notable antitumor activity, making it a valuable tool for studying caspase-related mechanisms in cancer research. Its ability to selectively inhibit caspase-4 can provide insights into therapeutic strategies aimed at mitigating inflammatory responses and promoting cell survival.
  8. Caspase-12 Inhibitor

    Z-ATAD-FMK is a selective inhibitor of caspase-12, playing a crucial role in modulating apoptotic processes triggered by endoplasmic reticulum stress. By inhibiting caspase-12 activity, Z-ATAD-FMK effectively reduces downstream activation of caspase-9, thereby interfering with the apoptotic signaling pathways. This compound is valuable for research applications investigating the mechanisms of ER stress-induced apoptosis and cellular responses to stress.
  9. RIPK2 Inhibitor

    RIPK2-IN-7 is a potent and selective inhibitor of RIPK2, exhibiting an IC50 of 0.6 nM. This compound effectively inhibits RIPK2 kinase activity, thereby disrupting the nucleotide-binding oligomerization domain (NOD) signaling pathway and decreasing the production of pro-inflammatory cytokines such as TNFα. RIPK2-IN-7 is a valuable tool for researching inflammatory bowel disease (IBD) and related inflammatory conditions.
  10. Caspase-1/4 Inhibitor

    VRT-043198 is a selective inhibitor of caspase-1 and caspase-4, functioning primarily as an interleukin-converting enzyme inhibitor. It demonstrates potent inhibition with Ki values of 0.8 nM for caspase-1 and 0.6 nM for caspase-4. This compound is capable of crossing the blood-brain barrier, making it valuable for research applications related to neuroinflammation and cytokine regulation.
  11. Caspase-3 Inhibitor

    Caspase-3-IN-1 is a potent inhibitor of caspase-3, exhibiting an IC50 of 14.5 nM. This compound plays a crucial role in the modulation of apoptotic signaling pathways, making it valuable for research in cell death mechanisms and therapeutic applications in cancer and neurodegenerative diseases. Its high specificity and efficacy allow for detailed studies on caspase-3 activity and its implications in various biological processes.
  12. Caspase Inhibitor

    Penicillic acid is a polyketide mycotoxin that serves as a caspase inhibitor. This compound demonstrates cytotoxic effects in rat alveolar macrophages, inhibiting Fas ligand-induced apoptosis through the blockade of caspase-8 self-processing. Its unique mechanism contributes to research in apoptosis and inflammation pathways, making it a valuable tool for studying cell death regulation in various biological contexts.
  13. Caspase-3 Inhibitor

    M826 is a selective, reversible non-peptide inhibitor of caspase-3, exhibiting an IC50 value of 0.005 μM. This compound demonstrates significant anti-apoptotic activity, both in vitro and in vivo, making it a valuable tool for studying apoptosis-related pathways. M826 is particularly relevant for research into nervous system diseases, offering potential insights into therapeutic strategies targeting apoptotic processes.
  14. p53 Activator/Wnt Inhibitor

    PAWI-2 is a p53 activator and Wnt inhibitor that targets β3-KRAS signaling independently of KRAS. This compound selectively inhibits the phosphorylation of TBK1, resulting in the activation of apoptotic pathways, evidenced by increased caspase-3/7 activity and PARP cleavage. Additionally, PAWI-2 facilitates the translocation of optineurin into the nucleus and induces G2/M cell cycle arrest. It effectively reverses cancer stemness and overcomes drug resistance in integrin β3 KRAS-dependent human pancreatic cancer stem cells, demonstrating significant tumor growth inhibition in orthotopic xenograft mouse models.
  15. Caspase Inhibitor

    Boc-Asp(OBzl)-CMK is a selective inhibitor of interleukin-1 converting enzyme (ICE, caspase-1). This compound effectively prevents cell death in CHP100 neuroblastoma cells and inhibits the release of IL-1β triggered by viral coat proteins. It serves as a valuable tool for researching inflammatory pathways and apoptotic processes in various biological contexts.
  16. Caspase Inhibitor

    IDN-1965 is an irreversible broad-spectrum inhibitor of caspases, crucial proteases involved in apoptosis. By inhibiting caspase activity, IDN-1965 effectively delays cytochrome c release and prevents downstream apoptotic processes, such as DNase activation. In preclinical studies, this compound has demonstrated a significant reduction in cardiomyocyte apoptosis, mitigating left ventricular dilation, systolic dysfunction, and fibrosis in models of dilated cardiomyopathy. IDN-1965 is valuable for research into apoptosis-related conditions, including heart failure and the underlying mechanisms of apoptosis initiation.
  17. Caspase-3/7 Inhibitor

    Ac-DNLD-CHO is a potent inhibitor of Caspase-3 and Caspase-7, exhibiting IC50 values of 9.89 nM and 245 nM, respectively, with corresponding Kiapp values of 0.68 nM and 55.7 nM. This reagent is valuable for investigating the role of caspase enzymes in apoptotic pathways and is particularly relevant in the study of diseases characterized by caspase-mediated cell death, including neurodegenerative disorders and viral infections. Researchers can utilize Ac-DNLD-CHO to explore therapeutic approaches targeting apoptosis in various health conditions.
  18. Caspase-3 Inhibitor

    M867 is a selective and reversible inhibitor of caspase-3, displaying an IC50 of 1.4 nM and a Ki of 0.7 nM. This compound demonstrates anti-apoptotic activity, making it a valuable tool for research focused on cell survival and apoptosis regulation. M867 is particularly relevant for studies exploring neurodegenerative diseases, cancer research, and therapeutic interventions targeting apoptotic pathways.
  19. Caspase Inhibitor

    Ac-YVAD-AOM is a selective inhibitor of caspase-1, a key enzyme involved in the inflammatory response and apoptosis. This compound demonstrates significant antitumor activity, making it a valuable tool for researchers studying cell death pathways and inflammatory diseases. Its specificity for caspase-1 enables detailed investigations into its role in various biological processes and therapeutic applications.
  20. Caspase Inhibitor

    Ac-YVAD-AMC is a potent caspase inhibitor that specifically targets the caspase-1 enzyme. It is widely used in research to study the mechanisms of apoptosis and inflammation, particularly in investigations of hypersensitive response (HR) cells. By preventing caspase-mediated cell death, Ac-YVAD-AMC is valuable for elucidating the role of caspases in various biological processes and for exploring potential therapeutic strategies in diseases characterized by dysregulated apoptosis.
  21. Caspase-3/7 Inhibitor

    Caspase-3/7 Inhibitor I is a reversible inhibitor targeting caspase-3 and caspase-7, exhibiting Ki values of 60 nM and 170 nM, respectively. This compound effectively inhibits apoptosis in various cellular models, including Camptothecin-treated Jurkat cells and chondrocytes. It serves as a valuable tool for studying mechanisms of cell death and developing therapeutic strategies against apoptotic diseases.
  22. Caspase-3 Inhibitor

    Ac-DEVD-CMK is a selective and irreversible inhibitor of caspase-3, making it a valuable tool for research involving apoptosis. This compound effectively prevents apoptosis triggered by elevated glucose levels and the presence of Ingenol 3,20-dibenzoate. Ac-DEVD-CMK is suitable for diverse experimental applications aimed at studying apoptotic pathways and evaluating potential therapeutic interventions.
  23. MDM2 Inhibitor

    ASTX295 is a selective MDM2 inhibitor that effectively disrupts the MDM2-p53 interaction, exhibiting an IC50 of less than 1 nM. By activating wild-type TP53, ASTX295 induces the expression of key transcriptional targets, resulting in cell death. This compound promotes the transition of pancreatic cancer cells from senescence to apoptosis while modulating p53 and DNA damage biomarkers. ASTX295 is suitable for research applications in hematologic malignancies and pancreatic cancer.
  24. Etoposide/Obatoclax/Caspase-3 Inhibitor

    M190S is a selective inhibitor of Caspase-3, demonstrating significant protection against mitochondria-dependent apoptosis in both in vitro and in vivo models. This small molecule is poised to serve as an essential research tool for elucidating mechanisms of cell death and for the development of therapeutics that target mitochondria-dependent apoptotic pathways. M190S also exhibits favorable oral bioavailability and excellent brain permeability, enhancing its potential utility in neurological research applications.
  25. Caspase-1 Inhibitor

    Ac-Tyr-Val-Lys-Asp-aldehyde is a reversible caspase-1 inhibitor, primarily targeting the caspase-1 enzyme. This compound plays a significant role in increasing GATA1 levels and enhancing erythroid differentiation. It is particularly useful in research applications pertaining to anemias associated with chronic diseases, chemotherapy-induced anemia, and Diamond-Blackfan anemia.
  26. Caspase-4 Inhibitor

    Ac-LEVD-CHO is a potent inhibitor of caspase-4, designed to selectively target this key protease involved in the apoptotic pathway. This peptide, comprising the sequence Ac-Leu-Glu-Val-Asp-al, effectively blocks caspase-4 activity, making it valuable for studies investigating apoptosis and inflammation. It serves as a useful tool for researchers examining the role of caspases in various biological processes and potential therapeutic interventions in related diseases.
  27. Caspase-1 Inhibitor

    CZL55 is a potent inhibitor of caspase-1, exhibiting an IC50 value of 24 nM. It plays a crucial role in modulating inflammatory pathways and apoptosis, making it valuable for studies related to febrile seizures (FS). This compound is useful for researchers investigating the underlying mechanisms of caspase-1 mediated processes in various pathological conditions.
  28. Caspase3 Inhibitor

    (Rac)-M826 is a selective and reversible inhibitor of caspase-3, exhibiting an IC50 value of 0.005 μM. This compound effectively inhibits apoptosis in NT2 cells, making it a valuable tool for research into nervous system diseases. Its specificity for caspase-3 positions it as a significant reagent for studies related to cell survival and neurodegenerative conditions.
  29. Caspase Inhibitor

    Z-Asp-CH2-DCB is an irreversible inhibitor targeting caspases, with broad-spectrum activity against proteases possessing caspase-like functions. This compound effectively blocks the production of pro-inflammatory cytokines such as IL-1β, TNF-α, IL-6, and IFN-γ in staphylococcal enterotoxin B-stimulated peripheral blood mononuclear cells, while also reducing SEB-induced T-cell proliferation in a dose-dependent manner. Additionally, Z-Asp-CH2-DCB mitigates SU5416-induced septal cell apoptosis and the development of emphysema, making it a valuable tool in apoptosis and inflammatory research applications.
  30. Caspase-10 Inhibitor

    Z-AEVD-FMK is a specific inhibitor of caspase-10, playing a critical role in the regulation of apoptosis. By inhibiting caspase-10, Z-AEVD-FMK effectively prevents the activation of Bid and the subsequent release of apoptosis-inducing factor (AIF) from mitochondria. This action leads to a notable reduction in apoptotic cell populations, making it a valuable tool for investigating apoptotic pathways and potential therapeutic interventions in related diseases.
  31. Caspase Inhibitor

    Z-VAD is an irreversible pan-caspase inhibitor that targets multiple caspases, including caspase-3, -6, -7, -8, and -9, while exhibiting a lesser inhibitory effect on caspase-2. This compound is utilized in research for its ability to block apoptosis signaling pathways, promote autophagy and necrosis in tumor cells, and exhibit anti-angiogenic properties. Z-VAD enhances the sensitivity of breast and lung cancer cells to radiotherapy, both in vitro and in vivo, and extends growth delay in tumor xenograft models. It is primarily employed in studies focused on cancer radiosensitization and the regulation of cell death pathways.
  32. Caspase 8 Inhibitor

    Caspase 8 Inhibitor CASP8-IN-1 (Compound 63-R) selectively inhibits caspase 8 with an IC50 value of 0.7 μM. This compound is effective in blocking FasL-induced apoptosis in Jurkat cells, making it a valuable tool for studying apoptotic signaling pathways and cellular responses to death stimuli. Its specificity and potency make CASP8-IN-1 suitable for research applications in cancer biology and therapeutic development targeting caspase-mediated cell death.
  33. α-mannosidase inhibitor

    Swainsonine (also known as Tridolgosir) is a naturally occurring indolizidine alkaloid and a potent, reversible inhibitor of α-mannosidase. By interfering with glycoprotein processing, Swainsonine disrupts key cellular signaling pathways, leading to apoptosis and G₂/M phase cell cycle arrest. It exhibits significant antitumor activity and has been widely studied for its potential role in cancer therapeutics and glycosylation-related biological processes.
  34. RAS(ON) Inhibitor

    Daraxonrasib (RMC-6236) is an orally active, non-covalent RAS(ON) inhibitor that disrupts the interaction between wild-type or mutant RAS proteins and the RAS-binding domain of BRAF. It exhibits EC₅₀ values ranging from 28 to 220 nM across wild-type KRAS, NRAS, HRAS, and multiple oncogenic RAS variants. RMC-6236 inhibits pERK signaling and demonstrates anti-tumor activity in KRAS-mutant tumor models.

  35. BRD4-p53 inhibitor

    SDU-071 is a potent, orally active inhibitor targeting the BRD4-p53 interaction. It inhibits the proliferation of MDA-MB-231 cells with an IC₅₀ of 10.5 μM and induces cell cycle arrest and apoptosis.
  36. EZH2/BRD4 inhibitor

    YM458 is a potent dual inhibitor of EZH2 and BRD4, with IC₅₀ values of 490 nM and 34 nM, respectively. It suppresses cell proliferation and colony formation, and induces cell cycle arrest and apoptosis in solid tumor cells. YM458 is suitable for anticancer research.
  37. CECR2 inhibitor

    NVS-CECR2-1 is a potent and selective non-BET family bromodomain (BRD) inhibitor targeting cat eye syndrome chromosome region, candidate 2 (CECR2). It binds CECR2 BRD with high affinity (IC50 = 47 nM; KD = 80 nM). NVS-CECR2-1 exhibits cytotoxic activity and induces apoptosis in various cancer cells through both CECR2-dependent and CECR2-independent mechanisms.
  38. Gαq/11/14 Inhibitor

    FR900359 is a cyclic depsipeptide and a selective inhibitor of Gαq/11/14 proteins in mammals. By targeting Gαq signaling, it effectively inhibits downstream pathways such as the ERK cascade. FR900359 has demonstrated the ability to suppress melanoma cell proliferation, lower blood pressure, and protect against airway hyperreactivity in murine models of allergen sensitization, such as the ovalbumin-induced asthma model.
  39. LSD1 inhibitor

    Bomedemstat (IMG-7289) is an orally active, irreversible inhibitor of lysine-specific demethylase 1 (LSD1). By inhibiting LSD1, it increases methylation of histone marks H3K4 and H3K9, leading to altered gene expression. Bomedemstat exhibits potent anti-cancer activity by inhibiting cancer cell proliferation and inducing apoptosis, and is being explored as a therapeutic agent in hematologic malignancies and other cancers.
  40. Menin-KMT2A inhibitor

    Bleximenib (JNJ-75276617) is an orally active and highly selective menin–KMT2A (MLL) interaction inhibitor, with IC50 values of 0.1 nM in humans, 0.045 nM in mice, and ≤0.066 nM in dogs. It effectively inhibits the proliferation of tumor cells and induces apoptosis and differentiation, particularly in malignancies driven by KMT2A rearrangements. Bleximenib is a promising therapeutic candidate for the study and treatment of leukemia and other menin-dependent cancers.
  41. Menin-KMT2A inhibitor

    Bleximenib (JNJ-75276617) oxalate is an orally active and highly selective inhibitor of the menin–KMT2A (MLL) interaction, with IC50 values of 0.1 nM in humans, 0.045 nM in mice, and ≤0.066 nM in dogs. It effectively inhibits tumor cell proliferation and induces apoptosis and differentiation, particularly in cancers driven by KMT2A rearrangements. Bleximenib oxalate is a promising candidate for research in leukemia and other menin–KMT2A-dependent malignancies.
  42. Caspase-1 inhibitor

    Ac-YVAD-cmk (Caspase-1 Inhibitor II) is a selective, irreversible inhibitor of caspase-1 (also known as IL-1β converting enzyme, ICE). It exhibits potent neuroprotective and anti-inflammatory effects by suppressing the expression of proinflammatory cytokines IL-1β and IL-18. Ac-YVAD-cmk also inhibits pyroptosis, a form of inflammatory cell death, making it a valuable tool for studying inflammation-related diseases and neurodegenerative disorders.
  43. APE1/REF-1 redox inhibitor

    APX2009 is a specific inhibitor of APE1/REF-1 redox activity with demonstrated anticancer properties. It reduces the proliferation, migration, and invasion of breast cancer cells and induces apoptosis. APX2009 holds potential for targeted cancer therapy by disrupting redox-regulated transcription factors involved in tumor progression.
  44. Osteoclast formation inhibitor

    ABD56 is a bioactive compound that inhibits osteoclast formation and induces osteoclast apoptosis. Its mechanism of action involves suppression of the NFκB and ERK signaling pathways, making it a promising candidate for research in bone metabolism and osteolytic diseases.
  45. PGAM1 inhibitor

    HKB99 is an allosteric inhibitor of phosphoglycerate mutase 1 (PGAM1) that induces apoptosis and suppresses cell migration by inhibiting the formation of invasive pseudopodia. It increases oxidative stress, activates the JNK/c-Jun pathway, and downregulates AKT and ERK signaling. HKB99 is a promising compound for the study of non-small cell lung cancer (NSCLC).
  46. Endoplasmic Reticulum Stress Inhibitor

    Tauroursodeoxycholate (Tauroursodeoxycholic acid; TDUCA) dihydrate is an inhibitor of endoplasmic reticulum (ER) stress that significantly downregulates pro-apoptotic molecules, including caspase-3 and caspase-12. Additionally, it suppresses ERK signaling, contributing to its cytoprotective and anti-apoptotic effects.
  47. EGFR inhibitor

    Avitinib (Abivertinib) maleate is a third-generation, irreversible, and orally active selective EGFR inhibitor with IC50 values of 0.18 nM for both EGFR^L858R and EGFR^T790M, and 7.68 nM for wild-type EGFR. In addition to its EGFR-targeting activity, Avitinib maleate also inhibits BTK phosphorylation and induces apoptosis in mantle cell lymphoma models, demonstrating broad-spectrum anticancer efficacy.
  48. CBSI inhibitor

    MY-673 is a colchicine binding site inhibitor (CBSI) that disrupts microtubule dynamics by inhibiting tubulin polymerization. In addition to its antimitotic effects, MY-673 suppresses the ERK signaling pathway, which leads to modulation of SMAD4 protein expression within the TGF-β/SMAD signaling axis. These combined actions result in potent inhibition of cancer cell proliferation and migration, and the induction of apoptosis, both in vitro and in vivo. MY-673 holds promise as a therapeutic candidate for targeting cancers driven by aberrant microtubule dynamics and dysregulated TGF-β/ERK signaling.
  49. phospholipase A2/HDAC2 inhibitor

    Rhamnetin is a naturally occurring flavonoid and quercetin derivative found in *Coriandrum sativum*. It functions as an inhibitor of secretory phospholipase A₂ and histone deacetylase 2 (HDAC2), contributing to its broad pharmacological profile. Rhamnetin exhibits notable antitumor, antioxidant, and anti-inflammatory activities, making it a promising compound for research in cancer, oxidative stress-related conditions, and inflammatory diseases.
  50. HDAC inhibitor

    Alteminostat (CKD-581) is a potent, broad-spectrum histone deacetylase (HDAC) inhibitor that targets both class I and class II HDAC isoforms. It promotes histone H3 and α-tubulin acetylation, indicating effective inhibition of nuclear and cytoplasmic HDAC activity. Alteminostat is being investigated for its therapeutic potential in hematologic malignancies, including lymphoma and multiple myeloma, and serves as a valuable tool in epigenetic cancer research.

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