1. Signaling Pathways
  2. Apoptosis
  3. Apoptosis

Apoptosis

Apoptosis

Apoptosis is a distinctive form of cell death exhibiting specific morphological and biochemical characteristics, including cell membrane blebbing, chromatin condensation, genomic DNA fragmentation, and exposure of specific phagocytosis signaling molecules on the cell surface. Cells undergoing apoptosis differ from those dying through necrosis. Necrotic cells are usually recognized by the immune system as a danger signal and, thus, resulting in inflammation; in contrast, apoptotic death is quiet and orderly.

There are two major pathways of apoptotic cell death induction: The intrinsic pathway, also called the Bcl-2-regulated or mitochondrial pathway, is activated by various developmental cues or cytotoxic insults, such as viral infection, DNA damage and growth-factor deprivation, and is strictly controlled by the BCL-2 family of proteins. The extrinsic or death-receptor pathway is triggered by ligation of death receptors (members of the tumor necrosis factor (TNF) receptor family, such as Fas or TNF receptor-1 (TNFR1)) that contain an intracellular death domain, which can recruit and activate caspase-8 through the adaptor protein Fas-associated death domain (FADD; also known as MORT1) at the cell surface. This recruitment causes subsequent activation of downstream (effector) caspases, such as caspase-3, -6 or -7, without any involvement of the BCL-2 family.

Studies suggest that alterations in cell survival contribute to the pathogenesis of a number of human diseases, including cancer, viral infections, autoimmune diseases, neurodegenerative disorders, and AIDS (acquired immunodeficiency syndrome). Treatments designed to specifically alter the apoptotic threshold may have the potential to change the natural progression of some of these diseases.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-144796
    VEGFR-2-IN-15
    Inducer
    VEGFR-2-IN-15 (Compound 14b) is a potent VEGFR-2 inhibitor. VEGFR-2-IN-15 arrests the HepG2 cell growth at the Pre-G1 phase and induces apoptosis.
    VEGFR-2-IN-15
  • HY-172880
    PLK1-IN-15
    Inducer
    PLK1-IN-15 (Compound 7n) is a PLK1 inhibitor (IC50: 38.5 nM). PLK1-IN-15 exhibits antiproliferative activity against HepG2, Huh7, H1299 and A549 cells (IC50: 2.03, 2.08, 4.79 and 17.11 μM, respectively). PLK1-IN-15 induces cell cycle arrest at the G2/M phase and apoptosis, and has anticancer activity.
    PLK1-IN-15
  • HY-17598R
    Rafoxanide (Standard)
    Inducer
    Rafoxanide (Standard) is the analytical standard of Rafoxanide. This product is intended for research and analytical applications. Rafoxanide is a poent, orally active halogenated salicylaniline agent with antiparasitic activity. Rafoxanide interferes with energy metabolism in trematodes by uncoupling oxidative phosphorylation. Rafoxanide is also found to be a potent inhibitor of the BRAF V600E mutant protein, which is important in colorectal cancer. Rafoxanide can be used for the control of infestation with Hemonchus species or Fasciola species in sheep and cattle as well as Oestrus ovis in sheep. Rafoxanide can also be used for cancer research.
    Rafoxanide (Standard)
  • HY-183353
    Nrf2 activator-25
    Inhibitor
    Nrf2 activator-25 is a Nrf2 activator. Nrf2 activator-25 promotes the dissociation of Nrf2 from Keap1 (with a Kd of 21.3 μM for Keap1), drives Nrf2 nuclear translocation, and increases the production of downstream antioxidant enzymes. Nrf2 activator-25 inhibits apoptosis, ferroptosis and vascular fibrosis, and protects vascular endothelial cells from damage. Nrf2 activator-25 can be used in the research of diabetic vascular diseases.
    Nrf2 activator-25
  • HY-155246
    PARP1-IN-15
    Inducer
    PARP1-IN-15 (Compound 6) is a PARP1 inhibitor. PARP1-IN-15 inhibits tankyrase (TNKS) and facilitates DNA double-strand breaks damage. PARP1-IN-15 induces tumor cell apoptosis. PARP1-IN-15 has anti-cancer activity in triple-negative breast cancer (TNBC) cells and TNBC patient-derived organoids. PARP1-IN-15 can be used for research of TNBC with or without BRCA1 mutations.
    PARP1-IN-15
  • HY-B0114S1
    Oxcarbazepine-d4-1
    Activator
    Oxcarbazepine-d4-1 is deuterium labeled Oxcarbazepine. Oxcarbazepine is a sodium channel blocker. Oxcarbazepine significantly inhibits glioblastoma cell growth and induces apoptosis or G2/M arrest in glioblastoma cell lines. Anti-cancer and anticonvulsant effects.
    Oxcarbazepine-d<sub>4</sub>-1
  • HY-181928
    PARP1/c-Met-IN-3
    Inducer
    PARP1/c-Met-IN-3 (Compound L19) is a selective c-Met and PARP1 inhibitor, with an IC50 of 5.4 nM against c-Met and an IC50 of 3.7 nM against PARP1. PARP1/c-Met-IN-3 inhibits PARP2 enzymatic activity with an IC50 of 4.52 nM, and shows no specificity for PARP1 and PARP2. PARP1/c-Met-IN-3 induces cell cycle arrest and apoptosis. PARP1/c-Met-IN-3 exhibits anti-tumor activity against triple-negative breast cancer.
    PARP1/c-Met-IN-3
  • HY-117281S1
    Moexipril-d3
    Inducer
    Moexipril-d3 is deuterated labeled Moexipril (HY-117281). Moexipril is an orally active inhibitor of angiotensin-converting enzyme (ACE), and becomes effective by being hydrolyzed to moexiprila hydrochloride. Moexipril exhibits antihypertensive and neuroprotective effects-.
    Moexipril-d<sub>3</sub>
  • HY-107314
    Pulchinenoside B
    Inducer
    Pulchinenoside B is a triterpenoid saponin isolated from Pulsatilla chinensis.
    Pulchinenoside B
  • HY-178032
    PARP1-IN-44
    Inducer
    PARP1-IN-44, an Olaparib (HY-10162) derivative, is an orally active PARP1 inhibitor (IC50 = 0.6 nM), and also inhibits PARP2 (IC50 = 1.0 nM) and PARP7 (IC50 = 7.5 nM). PARP1-IN-44 has selective antiproliferative activity against BRCA-deficient cancer cells with minimal toxicity to normal cells. PARP1-IN-44 induces G2/M phase arrest, promotes apoptosis, elevates ROS levels, disrupts mitochondrial membrane potential. PARP1-IN-44 suppresses PARylation while increasing γH2AX accumulation. PARP1-IN-44 activates the cGAS-STING pathway, upregulating IFN-β and CXCL10 expression. PARP1-IN-44 enhancing CD8+ T cell infiltration in a CT26 tumor mouse model, demonstrating robust in vivo antitumor efficacy.
    PARP1-IN-44
  • HY-N0069R
    Solamargine (Standard)
    Inducer
    Solamargine (Standard) is the analytical standard of Solamargine. This product is intended for research and analytical applications. Solamargine, a derivative from the steroidal solasodine in Solanum species, exhibits anticancer activities in numerous types of cancer. Solamargine induces non-selective cytotoxicity and P-glycoprotein inhibition. Solamargine significantly inhibits migration and invasion of HepG2 cells by down-regulating MMP-2 and MMP-9 expression and activity.
    Solamargine (Standard)
  • HY-181087
    Anticancer agent 296
    Inducer
    Anticancer agent 296 is a potent anticancer agent that activates the PERK-eIF2α-CHOP signaling pathway to induce endoplasmic reticulum stress, thereby regulating caspase and Bcl-2 family proteins, ultimately leading to apoptosis. Anticancer agent 296 increases intracellular levels of reactive oxygen species (ROS), reduces mitochondrial membrane potential, and promotes Ca2+ release. Anticancer agent 296 suppresses cell colony formation and S-phase cell proliferation, and induces autophagy. Anticancer agent 296 is applicable for research on non-small cell lung cancer (NSCLC).
    Anticancer agent 296
  • HY-W584515
    Thalidomide-NH-(CH2)3-NH-Boc
    Inducer
    Thalidomide-NH-(CH2)3-NH-Boc is a Boc-modified Thalidomide (HY-14658), which acts as a Cereblon ligand to recruit CRBN protein. The Boc protecting group at the end of Thalidomide-NH-(CH2)3-NH-Boc can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-NH-(CH2)3-NH-Boc is a key intermediate in the synthesis of CRBN-based designed PROTAC molecules targeting 11β-substituted estradiol.
    Thalidomide-NH-(CH2)3-NH-Boc
  • HY-139865
    142I5
    Antagonist
    142I5 is a potent ML-IAP Lys-covalent inhibitor with an IC50 value of 11 nM.
    142I5
  • HY-181871
    DZX19
    Inducer
    DZX19 (Compound C02) is an orally active, selective TRK inhibitor with a TRKA IC50 value of 1.32 nM, a TRKB IC50 of 2.28 nM, and a TRKC IC50 of 4.05 nM. DZX19 inhibits the kinase activities of wild-type TRKA, TRKA mutants (G595R, F589L, G667C), wild-type TRKB, and wild-type TRKC, and suppresses the phosphorylation of TRKA as well as its downstream AKT and ERK signaling pathways. DZX19 induces apoptosis. DZX19 inhibits tumor growth in a colorectal cancer xenograft mouse model. DZX19 is applicable for the research of colorectal cancer.
    DZX19
  • HY-173000
    STAT3-IN-40
    Inducer
    STAT3-IN-40 (Compound 8b) is an anti-cancer agent. STAT3-IN-40 can trigger the immune responses of CD4+ and CD8+ T lymphocytes and induce ferroptosis and apoptosis of tumor cells by inhibiting the expression and phosphorylation of STAT3. STAT3-IN-40 can be used in the research of chemoimmunotherapeutic agents for cancer.
    STAT3-IN-40
  • HY-N6253R
    Pinoresinol (Standard)
    Inducer
    Pinoresinol (Standard) is the analytical standard of Pinoresinol. This product is intended for research and analytical applications. Pinoresinol is a lignol of plant origin serving for defense in a caterpillar. Pinoresinol drastically sensitizes cancer cells against TNF-related apoptosis-inducing ligand (TRAIL) -induced apoptosis.
    Pinoresinol (Standard)
  • HY-178943
    Neuroprotective agent 15
    Inhibitor
    Neuroprotective agent 15 (Compound 3e) is a neuroprotective agent. Neuroprotective agent 15 is a selective butyrylcholinesterase (BChE) inhibitor, with IC50 values of 2.6 and 114.3 μM for BChE and AChE respectively. Neuroprotective agent 15 has cannabinoid CB2 receptor (CB2 receptor) agonistic activity. Neuroprotective agent 15 can reduce cell death, LDH release and Caspase-3/7 activity, and inhibit apoptosis. Neuroprotective agent 15 can reduce the formation of superoxide free radicals, maintain cell morphology, and significantly lower oxidative stress levels. Neuroprotective agent 15 can be used in the research of neurodegenerative diseases, such as Alzheimer's disease and Parkinson's disease.
    Neuroprotective agent 15
  • HY-163726
    GLUT1/EGFR-IN-1
    Inducer 99.75%
    GLUT1/EGFR-IN-1 (compound H) is a potent inhibitor of GLUT1 and EGFR. GLUT1/EGFR-IN-1 can simultaneously act on the EGFR tyrosine kinase ATP-binding site and inhibit GLUT1-mediated energy metabolism, resulting in reductions in ATP, MMP, intra-cellular lactic acid, and EGFR nuclear transfer. GLUT1/EGFR-IN-1 can be used for nasopharyngeal carcinoma (NPC) and triple-negative breast cancer (TNBC) research.
    GLUT1/EGFR-IN-1
  • HY-167701
    OBHSA
    OBHSA is a selective estrogen receptor (ERα) degrader. OBHSA blocks the cell cycle by degrading cyclin D1, thereby overcoming Tamoxifen (HY-13757A) resistance. OBHSA also triggers excessive activation of the unfolded protein response (UPR) by inducing an increase in intracellular reactive oxygen species, ultimately leading to cell apoptosis. In addition, OBHSA can also be used as an ERα ligand to synthesize PROTAC degraders.
    OBHSA
Cat. No. Product Name / Synonyms Application Reactivity