2. Signaling Pathways
  3. Apoptosis
  4. Apoptosis

Apoptosis

Apoptosis

Apoptosis

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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-182671
    SRX3305
    		Inducer
    SRX3305 is an BTK/PI3K/BRD4 inhibitor with IC50s of 6.5 nM, 15 nM, and 4 nM toward BTK, PI3Kɑ and PI3Kδ, respectively. SRX3305 attenuates chronic lymphocytic leukemia (CLL) and mantle cell lymphoma (MCL) cell proliferation and promotes apoptosis in a dose-dependent fashion. SRX3305 yields potent anti-tumor effects but spares healthy bystander cells. SRX3305 inhibits the activation-induced proliferation of primary CLL cells in vitro and effectively blocks microenvironment-mediated survival signals. SRX3305 blocks CLL cell migration toward CXCL-12 and CXCL-13. SRX3305 maintains its anti-tumor effects in Ibrutinib (HY-10997)-resistant CLL cells. SRX3305 can be used for research in CLL, diffuse large B-cell lymphoma (DLBCL) and MCL.
    SRX3305
  • HY-143246
    EGFR kinase inhibitor 1
    		Inducer
    EGFR kinase inhibitor 1 is a potent EGFR inhibitor with IC50s of 37, 1.7, >300 nM for WT, l885R/T790M, L858R/T790M/C797S, respectively. EGFR kinase inhibitor 1 induces apoptosis and cell cycle arrest at G0/G1-phase. EGFR kinase inhibitor 1 inhibits the cell motility. EGFR kinase inhibitor 1 shows antiproliferative and anti-tumor activity.
    EGFR kinase inhibitor 1
  • HY-P992291
    Anti-PL2L60 Antibody (KAO3)
    		Inducer
    Anti-PL2L60 Antibody (KAO3) is a PL2L60-targeting antibody. Anti-PL2L60 Antibody (KAO3) binds to PL2L60 expressed on tumor cell surfaces, blocking its tumor-promoting functions. Anti-PL2L60 Antibody (KAO3) arrests tumor cell cycle and induces cancer cell apoptosis. Anti-PL2L60 Antibody (KAO3) activates complement to mediate tumor cell lysis. Anti-PL2L60 Antibody (KAO3) can be used for the research of lymphoma, breast cancer, lung cancer, cervical cancer, colon cancer, and melanoma[1].
    Anti-PL2L60 Antibody (KAO3)
  • HY-182758
    Topoisomerase I-IN-21
    		Inducer
    Topoisomerase I-IN-21 is a promising topoisomerase I inhibitor with an IC50 of 18.79 μM. Topoisomerase I-IN-21 shows higher selectivity toward cancer cells over normal CD8+ cells. Topoisomerase I-IN-21 induces G0/G1 cell cycle arrest and apoptosis. Topoisomerase I-IN-21 activates the cGAS-STING pathway, leading to enhanced immune gene expression. Topoisomerase I-IN-21 can be used for research on leukemia, non-small-cell lung, colon, central nervous system, melanoma, ovarian, renal, prostate, and breast cancers.
    Topoisomerase I-IN-21
  • HY-178969
    GZD-257
    		Inducer
    GZD-257 is a brain-penetrant, ATP-competitive FAK inhibitor (IC50 = 14.3 nM), performing 4.77-fold selectivity with FAK to Pyk2 (IC50 = 68.2 nM). GZD-257 can significantly induce apoptosis of U118MG cells and arrest the cell cycle at the G2/M phase. GZD-257 can be used for the study of Glioblastoma (GBM).
    GZD-257
  • HY-N0331R
    Ziyuglycoside I (Standard)
    		Inducer
    Ziyuglycoside I (Standard) is the analytical standard of Ziyuglycoside I. This product is intended for research and analytical applications. Ziyuglycoside I isolated from S. officinalis root, has anti-wrinkle activity, and increases the expression of type I collagen. Ziyuglycoside I could be used as an active ingredient for cosmetics. Ziyuglycoside I triggers cell cycle arrest and apoptosis mediated by p53, it can be a potential agent candidate for treating triple-negative breast cancer (TNBC).
    Ziyuglycoside I (Standard)
  • HY-179140
    EGFR/VEGFR2-IN-8
    		Inhibitor
    EGFR/VEGFR2-IN-8 (compound 10k) is a dual EGFR/VEGFR-2 inhibitor (EGFR IC50 = 57 nM, VEGFR-2 IC50 = 21 nM). EGFR/VEGFR2-IN-8 has anti proliferative activity against various tumor cells, such as MCF-7 (IC50 = 20 nM), Panc-1 (IC50 = 22 nM), A-549 (IC50 = 23 nM), HT-29 (IC50 = 23 nM) cells. EGFR/VEGFR2-IN-8 has antioxidant and apoptosis inducing activity. EGFR/VEGFR2-IN-8 can be used for research on various types of cancer.
    EGFR/VEGFR2-IN-8
  • HY-146136
    EGFR-IN-56
    		Inducer
    EGFR-IN-56 (Compound 13a) is a potent EGFR inhibitor with IC50 values of 541.7 nM and 132.1 nM against EGFRT790M and EGFRT790M/L858R, respectively. EGFR-IN-56 blocks cancer cells in G2/M phase and induce into late apoptosis.
    EGFR-IN-56
  • HY-123786
    NSC745887
    		Inducer
    NSC745887 (compound 25) is an inhibitor that targets DNA topoisomerase cleavage, activates the caspase-8/9-caspase-3-poly (ADP-ribose) polymerase cascade, and induces apoptosis in cancer cells. NSC745887 enhances γH2AX expression and causes DNA fragmentation leading to DNA damage.
    NSC745887
  • HY-W144308R
    Tetrachlorohydroquinone (Standard)
    		Inhibitor
    Tetrachlorohydroquinone (Standard) is the analytical standard of Tetrachlorohydroquinone (HY-W144308). This product is intended for research and analytical applications. Tetrachlorohydroquinone (TCHQ) is a metabolite of Pentachlorophenol. Tetrachlorohydroquinone induces reactive oxidant stress (ROS), inhibits apoptosis and induces necrosis in primary mouse splenocytes. Tetrachlorohydroquinone increases DNA lesions and induces oxidative stress in rodents.
    Tetrachlorohydroquinone (Standard)
  • HY-N6016R
    Bacopaside II (Standard)
    		Inducer
    Bacopaside II (Standard) is the analytical standard of Bacopaside II. This product is intended for research and analytical applications. Bacopaside II, an extract from the medicinal herb Bacopa monnieri, blocks the Aquaporin-1 (AQP1) water channel and impairs migration of cells that express AQP1. Bacopaside II induces cell cycle arrest and apoptosis.
    Bacopaside II (Standard)
  • HY-121532
    (-)-Rasfonin
    		Inducer
    (-)-Rasfonin is a fungal secondary metabolite and inhibits small G proteins Ras. (-)-Rasfonin induces apoptosis, necrosis and autophagy in ACHN cells (a renal carcinoma cell line).
    (-)-Rasfonin
  • HY-184167
    COH-19
    		Inducer
    COH-19 is a potent mTOR inhibitor. COH-19 binds to the ATP-binding pocket of mTOR, reduces mTOR protein levels, and suppresses the PI3K/Akt/mTOR signaling pathway. COH-19 induces apoptosis via the mitochondrial pathway. COH-19 causes G0/G1 phase cell cycle arrest and suppresses cancer cell proliferation. COH-19 can be used for the research of breast cancer.
    COH-19
  • HY-161012
    RB-07-16
    		Inhibitor
    RB-07-16 is a C6-PyraP-BP inhibitor of human geranylammate pyrophosphate synthase (hGGPPS). RB-07-16 has antitumor activity.
    RB-07-16
  • HY-136489A
    KU-0058948 hydrochloride
    		Inducer
    KU-0058948 hydrochloride is a specific and potent PARP1 inhibitor with an IC50 of 3.4 nM. KU-0058948 hydrochloride induces cell cycle arrest and apoptosis of primary myeloid leukemic cells and myeloid leukemic cell lines.
    KU-0058948 hydrochloride
  • HY-W130288
    1-(1-Naphthyl)piperazine
    		Inducer
    1-(1-Naphthyl)piperazine is a 5-HT receptor modulator that acts as both a 5-HT2A receptor antagonist and 5-HT1A receptor agonist, and binds to human 5-HT6 receptor with a Ki of 120 nM. 1-(1-Naphthyl)piperazine partially inhibits forskolin-stimulated adenylate cyclase activity in calf substantia nigra. 1-(1-Naphthyl)piperazine inhibits UV-induced immunosuppression. 1-(1-Naphthyl)piperazine induces S-phase cell cycle delay, apoptosis and increases ROS levels, leading to inhibit MNT-1 cell proliferation. 1-(1-Naphthyl)piperazine can be used for melanoma research.
    1-(1-Naphthyl)piperazine
  • HY-149840
    Antitumor agent-113
    		Inducer
    Antitumor agent-113 shows cytotoxic effects on A549 cells with IC50 value of 46.60 μM and induces apoptosis. Antitumor agent-113 can be used in non-small cell lung cancer study.
    Antitumor agent-113
  • HY-176743
    Tubulin polymerization-IN-81
    		Inducer
    Tubulin polymerization-IN-81 is a selective Tubulin inhibitor with an IC50 of 5.41 μM. Tubulin polymerization-IN-81 possesses a significant anti-proliferative activity, unique ROS-mediated apoptotic mechanism and potent anti-microtubule activity. Tubulin polymerization-IN-81 can be used in anti-tumor research.
    Tubulin polymerization-IN-81
  • HY-145425
    PAIR2
    		Inducer
    PAIR2 is a highly selective inhibitor targeting the kinase domain of human IRE1α, with a Ki value of 8.8 nM against human IRE1α. PAIR2 fully occupies the ATP-binding site of the IRE1α kinase domain, partially antagonizes the ribonuclease activity of IRE1α, specifically inhibits regulated IRE1α-dependent decay (RIDD) and its mediated substrate cleavage, while preserving the splicing function of Xbp1 mRNA. PAIR2 also promotes the differentiation of B cells into plasma cells, blocks IRE1α-induced cell apoptosis, and restores the expression of Fgfr2 mRNA in AT2 cells. PAIR2 effectively reaches a steady-state concentration in the lung tissues of Mus musculus, and serves as an important tool for investigating the function of the IRE1α signaling pathway in diseases such as pulmonary fibrosis.
    PAIR2
  • HY-182447
    Contragestazol
    		Inducer
    Contragestazol (DL111-IT) is a non-hormonal antifertility agent. Contragestazol reduces the expression of Cyclin D1 and CDK4, increases the expression of total retinoblastoma protein (pRb), and decreases the level of hyperphosphorylated pRb. Contragestazol induces G0/G1 phase cell cycle arrest. Contragestazol inhibits embryonic development by inducing luteal cell apoptosis and reducing intrauterine polyamine levels. Contragestazol exhibits antitumor activity against prostate cancer, S180 tumor and H22 tumor. Contragestazol shows extremely potent activity in terminating early pregnancy in animals.
    Contragestazol
Cat. No. Product Name / Synonyms Application Reactivity