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-154861
    Anticancer agent 118
    Inducer
    Anticancer agent 118, a N‑acylated ciprofloxacin derivative, has anti-bacterial and anticancer activities. Anticancer agent 118 shows high activity against Gram-positive strains and antiproliferative activities against prostate PC3 cells. Anticancer agent 118 can be used for antitumor research.
    Anticancer agent 118
  • HY-183272
    PI3K/Akt/mTOR-IN-7
    Inhibitor
    PI3K/Akt/mTOR-IN-7 is an AKT/mTOR and JAK2/STAT3 inhibitor. PI3K/Akt/mTOR-IN-7 restores p-Akt, p-mTOR, and p-STAT3 expression, reduces pro-apoptotic Caspase-3 mRNA expression. PI3K/Akt/mTOR-IN-7 reduces intracellular ROS accumulation and inhibits NO production. PI3K/Akt/mTOR-IN-7 can be used for research on stroke, Alzheimer's disease and Parkinson's disease.
    PI3K/Akt/mTOR-IN-7
  • HY-113680
    KY1022
    KY1022 is a small molecule destabilizing Ras via targeting the Wnt/β-catenin pathway. KY1022 can inhibit cellular EMT, metastasis and apoptosis. KY1022 can be used for the research of metastatic colorectal cancer.
    KY1022
  • HY-B1121A
    Flunisolide hemihydrate
    Inducer
    Flunisolide hemihydrate is a corticosteroid, which is an orally active glucocorticoid receptor activator with anti-inflammatory activity. Flunisolide hemihydrate can induce eosinophil apoptosis, and is used for the research of asthma or rhinitis, and inflammation.
    Flunisolide hemihydrate
  • HY-182382
    Anticancer agent 311
    Inducer
    Anticancer agent 311 is an apoptosis inducer and p53 modulator. Anticancer agent 311 increases p53 levels, activates cleaved caspase-3, reduces p-Cdc25C levels, and disrupts p-p44/42 MAPK phosphorylation. Anticancer agent 311 induces G2/M phase arrest, inhibits cancer cell viability in a concentration- and time-dependent manner, and exhibits low toxicity to non-cancer cells. Anticancer agent 311 prevents tumor growth and angiogenesis in mouse xenograft models without detectable toxicity. Anticancer agent 311 can be used for the research of lung cancer.
    Anticancer agent 311
  • HY-N2632
    Uvarigrin
    Inducer
    Uvarigrin, isolated from the roots of Uvaria calamistrata, induces tumor multidrug resistance cell apoptosis and triggers Caspase-9 activation.
    Uvarigrin
  • HY-B0809B
    Theophylline sodium acetate
    Inducer
    Theophylline (1,3-Dimethylxanthine) sodium acetate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) sodium acetate inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) sodium acetate has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) sodium acetate induces apoptosis. Theophylline (1,3-Dimethylxanthine) sodium acetate can be used for asthma and chronic obstructive pulmonary disease (COPD) research.
    Theophylline sodium acetate
  • HY-173210
    TNF-α-IN-22
    Inducer
    TNF-α-IN-22 (Compound 30) is a TNFα inhibitor. It can induce Apoptosis by inhibiting the downregulation of IkBα induced by TNFα and blocking the cell cycle. TNF-α-IN-22 can be used in the research of triple-negative breast cancer.
    TNF-α-IN-22
  • HY-181664
    YCH3971
    Inducer
    YCH3971 is a PARP1 inhibitor with a PARP1 IC50 of 7.52 nM and a PARP1 EC50 of 67.75 nM. YCH3971 inhibits the proliferation of BRCA-deficient tumor cells. YCH3971 induces DNA damage, G2/M phase arrest, and caspase-mediated Apoptosis in triple-negative breast cancer cells. YCH3971 can be used for the research of BRCA-deficient tumors.
    YCH3971
  • HY-183351
    GN-604
    Inducer
    GN-604 is a targeted drug conjugate (Targeted Drug Conjugate, TDC) formed by conjugation of GNS561 (HY-137978) with DN604, a Pt (II) complex. GN-604 selectively inhibits PPT1, induces lysosomal dysfunction, suppresses autophagy and triggers apoptosis. GN-604 promotes the targeted sequestration of Pt (II) inside cells, induces DNA damage and inhibits the proliferation of malignant cells. GN-604 is applicable to research related to triple-negative breast cancer.
    GN-604
  • HY-P5142
    ω-Hexatoxin-Hv1a
    Inhibitor
    ω-Hexatoxin-Hv1a (ω-ACTX-Hv1; ω-Atracotoxin-HV1) is an orally active insecticidal neurotoxin containing an inhibitor cystine knot motif and a selective calcium channel inhibitor. ω-Hexatoxin-Hv1a blocks L-type voltage-dependent Ca2+ channels and reduces intracellular calcium ion concentration, thereby decreasing apoptosis, necroptosis and oxidative stress, and promoting cell recovery and energy level elevation. ω-Hexatoxin-Hv1a causes larval paralysis and death by impairing neurotransmission in the central nervous system of insects. It shows high injectable toxicity against insects of multiple orders, but exhibits weak oral toxicity. ω-Hexatoxin-Hv1a is widely applicable to studies related to ischemia-reperfusion injury, atopic dermatitis, and ischemic injury of cardiomyocytes and neurons.
    ω-Hexatoxin-Hv1a
  • HY-10984S
    Pomalidomide-d5
    Inducer
    Pomalidomide-d5 is deuterium labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.
    Pomalidomide-d<sub>5</sub>
  • HY-146817
    Tubulin polymerization-IN-11
    Inducer
    Tubulin polymerization-IN-11 is a potent tubulin polymerization inhibitor with an IC50 value of 3.4 μM. Tubulin polymerization-IN-11 shows antiproliferative activity. Tubulin polymerization-IN-11 induces Apoptosis and cell cycle arrest at G2/M phase. Tubulin polymerization-IN-11 decreases the expression of cyclin B1, p-cdc2, and Bcl-2 protein levels and increases the expression of cleaved PARP.
    Tubulin polymerization-IN-11
  • HY-181606
    Cyclo(phg-isoDGR-k)-PEG4-non-cleavable-SAR405838
    Inducer
    Cyclo (phg-isoDGR-k)-PEG4-non-cleavable-SAR405838 is a dual MDM2 and α5β1 integrin modulator. Cyclo (phg-isoDGR-k)-PEG4-non-cleavable-SAR405838 acts as an antiproliferative agent, apoptosis inducer and cell cycle regulator, induces reactivation of p53 and upregulation of p21, redistributes glioblastoma cells from the G0/G1 phase to the G2/M phase, and enhances apoptosis. Cyclo (phg-isoDGR-k)-PEG4-non-cleavable-SAR405838 is applicable to the research of glioblastoma.
    Cyclo(phg-isoDGR-k)-PEG4-non-cleavable-SAR405838
  • HY-138853A
    Thalidomide-NH-amido-C8-NH2 hydrochloride
    Inducer
    Thalidomide-NH-amido-C8-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-NH-amido-C8-NH2 hydrochloride
  • HY-182349
    Bax activator-2
    Inducer
    Bax activator-2 is a pro-apoptotic agent targeting BAX, with an IC50 of 0.30 μM against human BAX. Bax activator-2 binds to the trigger site of BAX and induces its conformational change. Bax activator-2 induces mitochondrial depolarization, cytochrome c release, cleavage of caspase-3/9 and PARP, thereby initiating apoptosis. Bax activator-2 exhibits cytotoxicity against a variety of cancer cell lines. Bax activator-2 can be used in research related to acute myeloid leukemia and solid tumors.
    Bax activator-2
  • HY-174445
    C199
    Inducer
    C199 is a PROTAC degrader targeting PRMT4 (DC50 = 106 nM). C199 shows high selectivity for PRMT4 over other protein arginile methyltransferases. C199 exhibits strong cell degradation ability. C199 induces apoptosis in MM cell lines. C199 efficiently clears PRMT4 protein via the VHL-proteasome pathway. C199 has a relatively long half-life and shows strong anti-multiple myeloma (MM) tumor activity (Pink: Target protein ligand (HY-111109); Blue: E3 ligase ligand (HY-112078), E3 ligase ligand + linker (HY-174474); black: Linker).
    C199
  • HY-157385
    HDAC-IN-67
    Inducer
    HDAC-IN-67 (compound 27f) is an HDAC inhibitor against HDAC1 and HDAC6, with IC50 values of 22 nM and 8 nM, respectively. HDAC-IN-67 inhibits cell proliferation and induces cell apoptosis. HDAC-IN-67 exhibits antitumor activity.
    HDAC-IN-67
  • HY-125570
    Ginsenoside Rs3
    Inducer
    Ginsenoside Rs3 is a natural diol-type ginseng saponin with anticancer effects. Ginsenoside Rs3 selectively elevates protein levels of p53 and p21WAF1 leading to induction of apoptosis in SK-HEP-1 cells.
    Ginsenoside Rs3
  • HY-156162
    Thalidomide-NH-C14-NH2 hydrochloride
    Inducer
    Thalidomide-NH-C14-NH2 hydrochloride is a Thalidomide (HY-14658)-based cereblon ligand that recruits CRBN proteins. Thalidomide-NH-C14-NH2 hydrochloride can be connected to the target protein ligand through a linker to form a PROTAC molecule. For example, THAL-SNS-032 (HY-123937).
    Thalidomide-NH-C14-NH2 hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity