Apoptosis

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  1. Caspase-3 Activator

    Dehydrotrametenolic acid is a sterol that activates caspase-3, playing a pivotal role in the induction of apoptosis. Isolated from the sclerotium of Poria cocos, this compound demonstrates significant anti-tumor activity, along with anti-inflammatory and anti-diabetic properties. Its mechanism and biological activities make it a valuable tool for research applications focused on apoptosis and potential therapeutic strategies against cancer and metabolic disorders.
  2. 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.
  3. Procaspase-3/6 Activator

    Procaspase-3/6 activator 1 is a highly selective activator of the executioner procaspases-3 and -6, exhibiting EC50 values of 2.4 ± 0.2 and 2.8 ± 0.3 μM, respectively. This compound does not activate procaspases-1 or -7, making it a valuable tool for investigating apoptotic processes. It is suitable for research applications focused on apoptosis, cell death mechanisms, and therapeutic development targeting caspase pathways.
  4. 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.
  5. Caspase-8 Substrate

    Ac-Ile-Glu-Thr-Asp-pNA is a substrate specifically designed for caspase-8. It features the Ile-Glu-Thr-Asp (IETD) peptide sequence, which is efficiently recognized and cleaved by caspase-8, resulting in the release of p-nitroaniline. The subsequent increase in p-nitroaniline concentration can be quantitatively measured through colorimetric detection at 405 nm, providing a reliable assay for evaluating caspase-8 enzymatic activity in various biological research applications.
  6. Apoptosis Inducer

    Polyporenic acid C is a lanostane-type triterpenoid that functions as an apoptosis inducer. Isolated from Poria cocos, this compound activates key apoptotic pathways by cleaving caspase-8, caspase-3, and PARP, while modulating the phosphorylation status of Akt, PTEN, and p53. Additionally, Polyporenic acid C enhances JNK activation and exhibits significant anticancer activity against non-small cell lung cancer. This makes it a valuable reagent for research into cancer therapies and apoptotic mechanisms.
  7. Caspase-6 Fluorogenic Substrate

    Ac-VEID-AFC is a fluorogenic substrate specifically designed for the detection of caspase-6 activity. Its cleavage by caspase-6 produces a fluorescent signal, making it a valuable tool for assessing apoptotic processes and related signaling pathways in various biological systems. This substrate is widely utilized in research applications focused on cell death, inflammation, and neurodegenerative diseases.
  8. Metacaspase Substrate

    Ac-VRPR-AMC is a fluorogenic substrate specifically designed for the detection of metacaspase activity. This compound is utilized in biochemical assays to measure metacaspase activity, making it a valuable tool for research in apoptosis and programmed cell death. Its fluorescence properties enable sensitive detection, facilitating studies on metacaspase function in various biological systems.
  9. Caspase Substrate

    Ac-LEVD-pNA is a chromogenic substrate that specifically targets caspase-4, facilitating the detection of its enzymatic activity. This compound is essential for studies related to apoptosis and cellular signaling pathways, providing a reliable assay tool for researchers investigating caspase-mediated processes in various biological contexts.
  10. 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.
  11. 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.
  12. 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.
  13. 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.
  14. 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.
  15. 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.
  16. 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.
  17. Apoptosis Inducer

    3-O-Methylgallic acid, a potent apoptosis inducer, is an anthocyanin metabolite known for its significant antioxidant properties. It effectively inhibits the proliferation of Caco-2 cells with an IC50 value of 24.1 μM, demonstrating its potential in cancer research. This compound is valuable for studying apoptotic pathways and therapeutic strategies in oncology.
  18. Caspase Activator

    5,7-Dihydroxychromone functions as a caspase activator and exhibits neuroprotective properties by activating the Nrf2/ARE signaling pathway. This compound effectively mitigates oxidative stress and apoptosis induced by 6-hydroxydopamine (6-OHDA) in SH-SY5Y cells. Additionally, 5,7-Dihydroxychromone reduces the expression of activated caspase-3, caspase-9, and cleaved PARP, making it a valuable tool for studying neuroprotection and apoptosis in cellular models.
  19. Caspase-9 Fluorogenic Substrate

    Ac-LEHD-AMC is a fluorogenic substrate specifically designed for the detection of caspase-9 activity. Upon hydrolysis by caspase-9, Ac-LEHD-AMC releases the AMC fluorophore, which emits fluorescence detectable at an excitation wavelength of 341 nm and an emission wavelength of 441 nm. This substrate is ideal for quantifying caspase-9 activity in various biological samples, facilitating research in apoptosis and related signaling pathways.
  20. Caspase-3 Activator

    Raptinal is a potent activator of caspase-3, directly initiating the intrinsic pathway of caspase-dependent apoptosis. By rapidly inducing cell death in cancer cells through the direct activation of effector caspase-3, Raptinal effectively bypasses the need for initiator caspase-8 and caspase-9 activation. This unique mechanism makes Raptinal a valuable tool for research in cancer therapy and apoptosis studies.
  21. 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.
  22. 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.
  23. SOS1 activator

    VUBI1 (SOS1 Activator 1) is a benzimidazole-derived small molecule that acts as a potent activator of the guanine nucleotide exchange factor SOS1, with a dissociation constant (Kᴅ) of 44 nM. It promotes RAS activation by enhancing RAS-GTP formation and modulates downstream ERK phosphorylation, thereby influencing RAS–MAPK signaling. In addition, VUBI1 serves as a functional ligand for the development of PROTAC-based degraders, such as PROTAC SOS1 Degrader-1, to induce targeted SOS1 degradation. VUBI1 is a valuable compound for studying RAS pathway regulation and its role in cancer biology.
  24. 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.
  25. ferroptosis inducer

    Solasonine is a naturally occurring steroidal glycoalkaloid isolated from *Solanum melongena* (eggplant), known for its anti-infective, anticancer, and neurogenesis-promoting properties. It acts as a ferroptosis inducer by disrupting the glutathione redox system through inhibition of glutathione peroxidase 4 (GPX4). By promoting ferroptotic cell death in hepatocellular carcinoma (HCC) cells, Solasonine serves as a valuable compound for investigating ferroptosis mechanisms and developing novel anticancer strategies.
  26. 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.

  27. IAP PROTAC degrader

    CST626 (Compound 9) is a pan-IAP degrader PROTAC that targets and degrades inhibitor of apoptosis proteins XIAP, cIAP1, and cIAP2 in MM.1S cells, with DC₅₀ values of 0.7 nM, 2.4 nM, and 6.2 nM, respectively.
  28. Solasodine (also known as Purapuridine) is a steroidal alkaloid found in plants of the Solanaceae family. It induces apoptosis by inhibiting the p53–MDM2 complex and downregulating p21^Waf1/Cip1 and Bcl-2 proteins. Solasodine exhibits a range of biological activities, including neuroprotective, antifungal, hypotensive, anticancer, antiatherosclerotic, antiandrogenic, and anti-inflammatory effects.
  29. 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.
  30. ENL PROTAC Degrader

    MS41 is a selective PROTAC degrader of eleven-nineteen leukemia (ENL), with DC₅₀ values of 3.50 nM (MV4;11), 2.84 nM (SEMK2), 3.03 nM (Jurkat), and 26.58 nM (KASUMI1). MS41 effectively inhibits the proliferation of ENL-dependent leukemia cells, induces G1 phase cell cycle arrest, and promotes apoptosis. It reduces chromatin occupancy of the ENL-associated transcription elongation complex, thereby suppressing oncogenic gene expression and leukemia progression.
  31. 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.
  32. 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.
  33. BRD4 Degrader

    TMX1 is a covalent molecular glue degrader targeting BRD4. It selectively recruits DCAF16 to the BRD4BD2 domain, inducing BRD4 degradation.
  34. 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.
  35. 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.
  36. 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.
  37. 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.
  38. 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.
  39. 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.
  40. L-Asparaginase (L-ASNase) is a deamidating enzyme that catalyses the hydrolysis of L-asparagine and L-glutamine, and can be used for the research of acute lymphoblastic leukemia. L-Asparaginase depletes L-asparagine from plasma resulting in inhibition of RNA and DNA synthesis with the subsequent blastic cell apoptosis.
  41. DNA Alkylator

    Illudin S is a natural sesquiterpene compound with potent cytotoxic, anti-tumor, and antiviral activities. It exhibits genotoxic effects and disrupts cell cycle progression by blocking the G1-S phase transition in human leukemia cells. Illudin S is of interest in cancer research due to its ability to target rapidly proliferating cells.
  42. 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.
  43. 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).
  44. 7-Hydroxyflavone is an orally active flavonoid isolated from *Clerodendrum phlomidis*, exhibiting notable anti-inflammatory activity. It protects renal cells from nicotine-induced cytotoxicity through activation of the ERK/Nrf2/HO-1 signaling pathway. Additionally, 7-Hydroxyflavone inhibits PKM2 with an IC50 of 2.12 μM, and suppresses COX-2 and 5-LOX with IC50 values of 27 μg/mL and 33 μg/mL, respectively.
  45. α-Amyrin is an orally active pentacyclic triterpenoid that activates the ERK and GSK-3β signaling pathways. It is studied for its potential in treating metabolic syndrome induced by a high-fructose diet and cognitive dysfunction associated with reduced cholinergic neurotransmission.
  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. DMU-212 is an orally active methylated derivative of Resveratrol that exhibits antimitotic, anti-proliferative, antioxidant, and pro-apoptotic activities. It induces mitotic arrest by promoting apoptosis and activating ERK1/2 signaling.
  48. mGluR5 allosteric modulator

    CDPPB is a selective, orally active allosteric modulator of the metabotropic glutamate receptor 5 (mGluR5). It enhances AKT and ERK1/2 signaling and upregulates BDNF mRNA expression. CDPPB also inhibits caspase-3 activation and mitigates mitochondrial dysfunction, demonstrating therapeutic potential in improving cognitive impairment, depression, and Huntington’s disease.
  49. TrkB activator

    HIOC is a potent and selective activator of the TrkB (tropomyosin receptor kinase B) receptor, capable of crossing both the blood-brain and blood-retinal barriers. It activates the TrkB/ERK signaling pathway, reduces neuronal apoptosis, and has been shown to attenuate early brain injury following subarachnoid hemorrhage (SAH). Additionally, HIOC exhibits neuroprotective effects in animal models of light-induced retinal degeneration.
  50. Apoptosis activator

    Sulforaphene, a natural compound isolated from radish seeds, exhibits an ED₅₀ of approximately 2 × 10⁻⁴ M against velvetleaf seedlings. It promotes apoptosis and inhibits migration in cancer cells by suppressing signaling pathways including EGFR, phosphorylated ERK1/2 (p-ERK1/2), and NF-κB.

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