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-15472A
    PRX-08066 maleate
    Inhibitor
    PRX-08066 maleate is a selective and orally active 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist with a Ki of 3.4 nM. PRX-08066 maleate inhibits the MAPK pathway, 5-HT release and fibrotic factor (TGFβ1, CTGF and FGF2) expression. PRX-08066 maleate inhibits the proliferation of KRJ-I cells and induces apoptosis (caspase-3 activation). PRX-08066 maleate inhibits pulmonary vascular remodeling. PRX-08066 maleate can be used of pulmonary Arterial Hypertension (PAH) and neuroendocrine tumor (NET).
    PRX-08066 maleate
  • HY-183801
    Cu2LCl2(H2O)
    Inducer
    Cu2LCl2(H2O) acts as a proteasome inhibitor and protein tyrosine phosphatase inhibitor, with antiproliferative and apoptosis-inducing effects. Cu2LCl2(H2O) exhibits low cytotoxicity against normal cells and remarkable in vivo antitumor efficacy. Cu2LCl2(H2O) inhibits proteasome activity in colon cancer cells, and suppresses PTP1B and TCPTP activities in breast cancer cells. Cu2LCl2(H2O) can be used in the research of colon cancer, breast cancer and liver cancer.
    Cu2LCl2(H2O)
  • HY-172399
    FTO-IN-14
    Inducer
    FTO-IN-14 (Compound F97) is the inhibitor for the RNA demethylase Fat mass and obesity-associated protein FTO with IC50 of 0.45 μM. FTO-IN-14 regulates the protein expression of ASB2, RARA and MYC. FTO-IN-14 exhibits antiproliferative activity in AML cancer cells (IC50 for MOLM13, NB4, HEL, OCI-AML3, MV4-11 and MONOMAC6 is 0.7-5.5 μM), induces apoptosis in NB4 cell. FTO-IN-14 exhibits antitumor activity in mouse NB4 xenograft models.
    FTO-IN-14
  • HY-169299
    TOPOI/PARP-1-IN-2
    Inducer
    TOPOI/PARP-1-IN-2 (compound 6c) is a dual PARP-1 and topoisomerase 1 (TOPO-1) inhibitor with IC50s of 32.2 nM and 46.2 nM, respectively. TOPOI/PARP-1-IN-2 shows a selectivity for PARP-1 over PARP-2. TOPOI/PARP-1-IN-2 disrupts the cell cycle at the S phase and induces apoptosis in NCI-60 cancer cell lines.
    TOPOI/PARP-1-IN-2
  • HY-N0410R
    Daucosterol (Standard)
    Inducer
    Daucosterol (Standard) is the analytical standard of Daucosterol. This product is intended for research and analytical applications. Daucosterol is an orally active natural sterol compound, which has anti-inflammatory, anticancer and immunomodulatory activities. Daucosterol inhibits cancer cell proliferation by inducing autophagy through ROS-dependent manner. Daucosterol also inhibits colon cancer growth by inducing apoptosis, inhibiting cell migration and invasion and targeting caspase signalling pathway.
    Daucosterol (Standard)
  • HY-183590
    CAIX/XII-IN-17
    Inducer
    CAIX/XII-IN-17 is a selective human carbonic anhydrase IX/XII (CA IX/XII) inhibitor with Ki values of 25.1 nM (hCA IX) and 35.2 nM (hCA XII). CAIX/XII-IN-17 induces apoptosis in pancreatic cancer cells. CAIX/XII-IN-17 can be used for the research of breast cancer, pancreatic cancer.
    CAIX/XII-IN-17
  • HY-13434AR
    Ionomycin calcium (Standard)
    Inducer
    2-(1-Piperazinyl)pyrimidine (Standard) is the analytical standard of 2-(1-Piperazinyl)pyrimidine. This product is intended for research and analytical applications. 2-(1-Piperazinyl)pyrimidine is the major metabolite of Tandospirone (HY-14558).
    Ionomycin calcium (Standard)
  • HY-172919
    PDEδ/NAMPT IN-1
    Inducer
    PDEδ/NAMPT IN-1 (Compound 17d) is a dual inhibitor targeting phosphodiesterase 6 (PDE6) (KD=0.410 nM) and nicotinamide phosphoribosyl transferase (NAMPT) (IC50=2.21 nM). PDEδ/NAMPT IN-1 blocks KRAS-related signal transduction and interferes with the synthesis of nicotinamide adenine dinucleotide (NAD+), inducing apoptosis in KRAS mutant pancreatic cancer cells. PDEδ/NAMPT IN-1 is promising for research of KRAS mutant pancreatic cancer.
    PDEδ/NAMPT IN-1
  • HY-142570S1
    Nalmefene-d4
    Nalmefene-d4 is the deuterium labeled Nalmefene (HY-107744). Nalmefene is a BBB-penetrable?opioid receptor?modulator. Nalmefene is an antagonist of?MOR?and?DOR, and a partial agonist of?KOR. Nalmefene has anti-inflammatory and neuroprotective activities. Nalmefene can be used in the research of reducing alcohol-dependent disorders.
    Nalmefene-d<sub>4</sub>
  • HY-173034
    PTP1B-IN-30
    Inducer
    PTP1B-IN-30 (Compound 3j) is the inhibitor for PTP1B with an IC50 of 0.51 µM. PTP1B-IN-30 inhibits the proliferation of cancer cell T47D with an IC50 of 21.21 µM, arrests the cell cycle at S phase, and induces apoptosis in T47D.
    PTP1B-IN-30
  • HY-N6939R
    Pseudolaric Acid B (Standard)
    Inducer
    Pseudolaric Acid B (Standard) is the analytical standard of Pseudolaric Acid B. This product is intended for research and analytical applications. Pseudolaric Acid B is an orally active diterpene acid. Pseudolaric Acid B has anti-fungal, anti-fertility, anti-angiogenesis and anticancer activity, and can induce tumor cell apoptosis and autophagy. In addition, Pseudolaric Acid B can inhibit the secretion of hepatitis B virus (HBV) and has immunosuppressive effect, selectively inhibiting the proliferation of T lymphocytes and the production of IL-2.
    Pseudolaric Acid B (Standard)
  • HY-150755
    Topo I/COX-2-IN-2
    Inducer
    Topo I/COX-2-IN-2 (Compound W10) is a potent dual-target inhibitor of Topo I and COX-2 with IC50 values of 0.90 μM and 2.31 μM, respectively. Topo I/COX-2-IN-2 induces cancer cell apoptosis through the mitochondrial pathway.
    Topo I/COX-2-IN-2
  • HY-P992391
    IPH4301
    Inducer
    IPH4301 is a monoclonal antibody targeting MICA/B, with dual activities of cytotoxicity and immunoregulation. IPH4301 blocks the interaction between MICA/B and NKG2D, inhibits their hydrolysis into soluble sMICA/B, and mediates antibody-dependent cellular cytotoxicity and antibody-dependent cellular phagocytosis against tumor cells expressing MICA/MICB. IPH4301 restores the expression and function of NKG2D on primary NK cells and T cells, reverses the immunosuppression induced by M2 macrophages, and enhances NK cell-mediated tumor cell apoptosis. IPH4301 can be used in research related to cancer and triple-negative breast cancer.
    IPH4301
  • HY-N0566R
    23-Hydroxybetulinic acid (Standard)
    Inducer
    23-Hydroxybetulinic acid (Standard) is the analytical standard of 23-Hydroxybetulinic acid (HY-N0566). This product is intended for research and analytical applications. 23-Hydroxybetulinic acid (Anemosapogenin) is an orally active triterpenoid with broad-spectrum anticancer activity. 23-Hydroxybetulinic acid reduces the levels of Bcl-2 and survivin, elevates the level of Bax, promotes the cleavage/activation of caspase-3 and caspase-9, and induces apoptosis via the endogenous mitochondrial pathway involving cytochrome C release and mitochondrial membrane potential disruption. 23-Hydroxybetulinic acid arrests the cell cycle at S and G1 phases, inhibits cancer cell proliferation, blocks the MAPK signaling pathway, regulates MMP2, and induces autophagic apoptosis by upregulating beclin-1. 23-Hydroxybetulinic acid inhibits the activity and efflux function of P-gp, increases the intracellular accumulation of chemotherapeutic drugs, and synergistically enhances cytotoxicity with Doxorubicin (HY-15142). 23-Hydroxybetulinic acid inhibits the phosphorylation and nuclear translocation of STAT6, blocks M2 macrophage polarization, and reduces M2 macrophage-mediated apoptosis resistance of colon cancer cells. 23-Hydroxybetulinic acid can be used in related studies on chronic myeloid leukemia, hepatocellular carcinoma, sarcoma 180, multidrug-resistant breast cancer, leukemia, Doxorubicin-induced cardiotoxicity, and colorectal cancer.
    23-Hydroxybetulinic acid (Standard)
  • HY-W015084R
    β-Ionone (Standard)
    Inducer
    β-Ionone (Standard) is the analytical standard of β-Ionone. This product is intended for research and analytical applications. β-Ionone is effective in the induction of apoptosis in gastric adenocarcinoma SGC7901 cells. Anti-cancer activity.
    β-Ionone (Standard)
  • HY-179143
    EGFR-IN-185
    Inducer
    EGFR-IN-185 is a EGFR inhibitor. EGFR-IN-185 exhibits potent activity against non-small cell lung cancer (NSCLC) cells harboring EGFR mutations. EGFR-IN-185 inhibits colony formation and migration, induces G0/G1 arrest, and promots apoptosis, which are associated with the suppression of EGFR and AKT phosphorylation. EGFR-IN-185 can be used for the research of  NSCLC.
    EGFR-IN-185
  • HY-N15637
    Torularhodin
    Inhibitor
    Torularhodin is a carotenoid with anti-cancer activity. Torularhodin induces apopotsis of tumor cells and can be used for the study of prostate cancer.
    Torularhodin
  • HY-146080
    Antitumor agent-61
    Activator
    Antitumor agent-61 (Compound 9b), Irinotecan (Ir) derivative, is a potential antitumor agent. Antitumor agent-61 displays potent activity with IC50s of 0.92, 1.39, 1.75, 2.20, 3.05 and 3.23 μM against five human cancer cells SK-OV-3, SK-OV-3/CDDP, U2OS, MCF-7, A549 and MG-63, respectively. Antitumor agent-61 induces SK-OV-3 cells apoptosis through mitochondrion pathways.
    Antitumor agent-61
  • HY-176288
    eIF4E/eIF4G PPI-IN-1
    Inducer
    eIF4E/eIF4G PPI-IN-1 is an eIF4E/eIF4G interaction inhibitor with a KD of 20.2 μM for eIF4E protein. eIF4E/eIF4G PPI-IN-1 plays an antitumor role in multiple modes of action including regulating the activity of eIF4E by inhibiting the Ras/MAPK/eIF4E signaling pathway, apoptosis and cell migration. eIF4E/eIF4G PPI-IN-1 suppresses the growth of HepG2 xenografts in nude mice and was relatively nontoxic to mice.
    eIF4E/eIF4G PPI-IN-1
  • HY-15025AS
    Sildenafil citrate-d8
    Sildenafil (citrate)-d8 is the deuterium labeled Sildenafil citrate. Sildenafil citrate is a potent phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 5.22 nM.
    Sildenafil citrate-d<sub>8</sub>
Cat. No. Product Name / Synonyms Application Reactivity